Inflammatory diseases

PHARMACEUTICAL COMPOSITION FOR PREVENTING OR TREATING ARTHRITIS OR INFLAMMATORY DISEASE CONTAINING 2-METHOXY-4-(3-(4-METHOXYPHENYL)PROPYL-1-EN-1-YL)PHENOL AS ACTIVE INGREDIENT
(Fri, 18 May 2018)
<p id="p-0001" num="0000">Disclosed herein is a pharmaceutical composition for treating or preventing inflammatory diseases or arthritis, which includes
2-methoxy-4-(3-(4-methoxyphenyl)prop-1-en-1-yl)phenol or a pharmaceutically acceptable salt thereof as an active ingredient. The pharmaceutical composition exhibits superior therapeutic efficacy
against arthritis without any side effects such as toxicity, etc.</p>
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1-PYRAZOLYL-3- (4- ((2 -ANILINOPYRIMIDIN- 4 - YL) OXY) NAPTHTHALEN- I - YL) UREAS AS P38 MAPKINASE INHIBITORS
(Fri, 18 May 2018)
<p id="p-0001" num="0000">There is provided a compound of formula (I) which is an inhibitor of the family of p38 mitogen-activated protein kinase enzymes, and to its use in therapy, including
in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, such as asthma and COPD.</p>
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NOVEL COMPOUNDS
(Fri, 18 May 2018)
<p id="p-0001" num="0000">The present invention relates to compounds, compositions, combinations and medicaments containing said compounds and processes for their preparation. The invention
also relates to the use of said compounds, combinations, compositions and medicaments, for example as inhibitors of the activity of RIP2 kinase, including degrading RIP2 kinase, the treatment of
diseases and conditions mediated by the RIP2 kinase, in particular for the treatment of inflammatory diseases or conditions.</p>
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INHIBITORS OF ALPHA-AMINO-BETA-CARBOXYMUCONIC ACID SEMIALDEHYDE DECARBOXYLASE
(Fri, 18 May 2018)
<p id="p-0001" num="0000">The present disclosure discloses compounds capable of modulating the activity of α-amino-β-carboxymuconic acid semialdehyde decarboxylase (ACMSD), which are useful for
the prevention and/or the treatment of diseases and disorders associated with defects in NAD<sup>+</sup> biosynthesis, e.g., metabolic disorders, neurodegenerative diseases, chronic
inflammatory diseases, kidney diseases, and diseases associated with ageing. The present application also discloses pharmaceutical compositions comprising said compounds and the use of such compounds
as a medicament.</p>
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BICYCLIC HETEROARYL DERIVATIVES AS MNK1 AND MNK2 MODULATORS AND USES THEREOF
(Thu, 17 May 2018)
The present invention relates to certain compounds (e.g., imidazopyrazine, imidazopyridine, imidazopyridazine and imidazpyrimidine compounds) that act as inhibitors of the MAP kinase interacting
kinases MNK2a, MNK2b, MNK1a, and MNK1b. The present invention further relates to pharmaceutical compositions comprising these compounds, and to the use of the compounds for the preparation of a
medicament for the prophylaxis and treatment of diseases (e.g., proliferative diseases (e.g., cancer), inflammatory diseases, Alzheimer's disease), as well as methods of treating these diseases.
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SERINE/THREONINE KINASE INHIBITORS
(Thu, 17 May 2018)
Compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof are provided, which are useful for the treatment of hyperproliferative, pain and inflammatory
diseases. Methods of using compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof, for in vitro , in situ , and in vivo diagnosis, prevention or
treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.
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EXTRACTS OF ANDROGRAPHIS PANICULATA, METHODS FOR PREPARATION AND USE THEREOF
(Sat, 12 May 2018)
Disclosed herein are extracts of Andrographis paniculata having highly concentrated active ingredients, preparation methods and medical use for treating autoimmunity and inflammatory disease.
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EXTRACTS OF ANDROGRAPHIS PANICULATA, METHODS FOR PREPARATION AND USE THEREOF
(Sat, 12 May 2018)
Disclosed herein are extracts of Andrographis paniculata having highly concentrated active ingredients, preparation methods and medical use for treating autoimmunity and inflammatory disease.
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PYRIDAZINE DERIVATIVES AS RORC MODULATORS
(Sat, 12 May 2018)
Compounds of formula (I): (I) or pharmaceutical salts thereof, wherein m, n,, p, q A, B, Ri, R2, R3, R4, R5, R6and R7are as defined herein. Also disclosed are methods of making the compounds and
using the compounds as RORs modulators for treatment of inflammatory diseases such as arthritis.
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NOVEL CHOLESTEROL METABOLITE, 5-CHOLESTEN, 3BETA-25-DIOL, DISULFATE (25HCDS) FOR THERAPY OF METABOLIC DISORDERS, HYPERLIPIDEMIA, DIABETES, FATTY LIVERS DISEASES AND ATHEROSCLEROSIS
(Fri, 11 May 2018)
<p id="p-0001" num="0000">5-cholesten, 3β,25-diol, disulfate (25HCDS) has been found to be an authentic PPARγ agonist and LXR antagonist, and is used for the therapy of lipid disorders and
inflammatory diseases, including without limitation fatty liver, inflammatory bowel, and atherosclerotic diseases.</p>
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TERT-BUTYL N-[2-{4-[6-AMINO-5-(2,4-DIFLUOROBENZOYL)-2-OXOPYRIDIN-1(2H)-YL]-3,5- DIFLUOROPHENYL}ETHYL]-L-ALANINATE OR A SALT,HYDRATE OR SOLVATE THEREOF
(Fri, 11 May 2018)
<p id="p-0001" num="0000">The present invention provides a compound which is: tert-butyl N-[2-{4-[6-amino-5-(2,4-difluorobenzoyl)-2-oxopyridin-1(2H)-yl]-3,5-difluorophenyl}ethyl)-L-alaninate or
a salt, hydrate or solvate thereof. The present invention also provides a pharmaceutical composition comprising the compound together with one or more pharmaceutically acceptable carriers and/or
excipients. The compound and composition are useful for inhibiting the activity of a p38 MAP kinase enzyme. As such they may be used in the treatment of a autoimmune or inflammatory disease, or a
cell proliferative disease. In addition, the invention provides an acid produced by hydrolysis of the ester group of the compound of the invention. The acid is
N-[2-{4-[6-amino-5-(2,4-difluorobenzoyl)-2-oxopyridin-1(2H)-yl]-3,5-difluorophenyl}ethyl)-L-alanine.</p>
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SERINE/THREONINE KINASE INHIBITORS
(Fri, 11 May 2018)
<p id="p-0001" num="0000">Compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof are provided, which are useful for the treatment of
hyperproliferative, pain and inflammatory diseases. Methods of using compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof, for in vitro, in situ,
and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.</p> <p id="p-0002" num="0000"><chemistry
id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="29.29mm" wi="62.06mm" file="US20180127393A1-20180510-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/>
</chemistry> </p>
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lAP E3 LIGASE DIRECTED PROTEOLYSIS TARGETING CHIMERIC MOLECULES
(Fri, 04 May 2018)
<p id="p-0001" num="0000">The present invention relates to compounds, compositions, combinations and medicaments containing said compounds and processes for their preparation. The invention
also relates to the use of said compounds, combinations, compositions and medicaments, for example as inhibitors of the activity of RIP2 kinase, including degrading RIP2 kinase, the treatment of
diseases and conditions mediated by the RIP2 kinase, in particular for the treatment of inflammatory diseases or conditions.</p>
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NEW COMPOUNDS I
(Fri, 04 May 2018)
<p id="p-0001" num="0000">The present invention relates to compounds of formula (I),</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img
id="EMI-C00001" he="24.21mm" wi="60.28mm" file="US20180118744A1-20180503-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003"
num="0000">and their pharmaceutically acceptable salts, solvates, hydrates, geometrical isomers, tautomers, optical isomers or N-oxides, which are inhibitors of SSAO activity. The invention
further relates to pharmaceutical compositions comprising these compounds and to the use of these compounds for the treatment of medical conditions wherein inhibition of SSAO activity is beneficial,
such as inflammatory diseases and immune disorders.</p>
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COMPOUNDS
(Fri, 04 May 2018)
<p id="p-0001" num="0000">The present invention relates to compounds of formula (I)</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img
id="EMI-C00001" he="65.45mm" wi="69.85mm" file="US20180118754A1-20180503-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003"
num="0000">and to compositions comprising the same and to the use of the compounds and their compositions in treatment, for example in the treatment of inflammatory diseases, in particular
respiratory inflammatory disease. The invention also extends to methods of making said compounds.</p>
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NOVEL COMPOUND HAVING IMMUNE DISEASE TREATMENT EFFECT AND USE THEREOF
(Fri, 04 May 2018)
<p id="p-0001" num="0000">The present invention relates to a novel compound capable of effectively preventing and treating immune diseases and a use thereof. The novel compound of the present
invention has effects of inhibiting the production of inflammatory cytokines, increasing the activity of regulatory T cells having immunoregulatory functions, inhibiting the production of
auto-antibodies to regulate excessive immune responses, and inhibiting the differentiation of osteoclasts, and thus can be used for treating immune diseases, such as autoimmune disease, inflammatory
disease, and transplant rejection diseases, which are caused by abnormal regulation of various kinds of immune response</p>
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PYRAZOLYL UREAS AS KINASE INHIBITORS
(Fri, 04 May 2018)
<p id="p-0001" num="0000">There are provided compounds of formula (I) as defined in the specification which are p38 MAP kinase inhibitors for use as medicaments for the treatment inter alia of
inflammatory diseases.</p>
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N,N'-DIARYLUREA, N,N'-DIARYLTHIOUREA AND N,N'-DIARYLGUANIDINO COMPOUNDS FOR USE IN TREATMENT AND PREVENTION OF INFLAMMATORY DISEASE
(Fri, 04 May 2018)
A compound according to formula (I) wherein L is CH2−O, CH2−S, CH2−CH2, or CH=CH; R1 and R2 are independently selected out of H, halogen, C1 to C3 alkyl, halogenated C1 to C3 alkyl, C1 to C3
alkyloxy, or halogenated C1 to C3 alkyloxy; Ar is an aryl moiety, preferably phenyl or naphthyl, or a moncyclic- or bicyclic heteroaryl moiety, wherein optionally the aryl or heteroaryl moiety is
further substituted; X is O, S, or NR3, wherein R3 is H, C1 to C3 alkyl, halogenated C1 to C3 alkyl, or tert-butyloxycarbonyl; Y is O, S, NR4 or N(R4)R5, wherein R4 and R5 are independently selected
out of H or C1 to C3 alkyl; and wherein if Y is O, S, or NR4, then both A are NH, and the punctuated bonds represent a double bond to Y and single bonds to each A; or wherein if Y is N(R4)R5, then
one A is N, the other A is NH, and the punctuated bonds represent a double bond to the A being N, a single bond to the A being NH and a single bond to Y; and use of such a compound in treatment or
prevention of an inflammatory disease or an inflammation-related disorder.
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N,N' -DIARYLUREA, N,N' -DIARYLTHIOUREA AND N,N' -DIARYLGUANIDINO COMPOUNDS FOR USE IN TREATMENT AND PREVENTION OF INFLAMMATORY DISEASE
(Thu, 03 May 2018)
A compound according to formula I wherein L is CH 2 -O, CH 2 -S, CH 2 -CH 2 , or CH=CH; R 1 and R 2 are independently selected out of H, halogen, C1 to C3 alkyl, halogenated C1 to C3 alkyl, C1 to C3
alkyloxy, or halogenated C1 to C3 alkyloxy; Ar is an aryl moiety, preferably phenyl or naphthyl, or a moncyclic- or bicyclic heteroaryl moiety, wherein optionally the aryl or heteroaryl moiety is
further substituted; X is O, S, or NR 3 , wherein R 3 is H, C1 to C3 alkyl, halogenated C1 to C3 alkyl, or tert -butyloxycarbonyl; Y is O, S, NR 4 or N(R 4 )R 5 , wherein R 4 and R 5 are
independently selected out of H or C1 to C3 alkyl; and wherein if Y is O, S, or NR 4 , then both A are NH, and the punctuated bonds represent a double bond to Y and single bonds to each A; or wherein
if Y is N(R 4 )R 5 , then one A is N, the other A is NH, and the punctuated bonds represent a double bond to the A being N, a single bond to the A being NH and a single bond to Y; and use of such a
compound in treatment or prevention of an inflammatory disease or an inflammation-related disorder.
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METHODS FOR THE TREATMENT AND PREVENTION OF INFLAMMATORY DISEASES
(Fri, 20 Apr 2018)
<p id="p-0001" num="0000">The inventors demonstrate that treatment of young, suckling mice with a glycolipid derived from <i>Helicobacter pylori </i>activates NKT cells in a
CD1d-restricted fashion, and is protective against AHR in a model of allergen-induced asthma. The inventors further found that this protective effect can be transferred by NKT cells exposed to the
glycolipid, and is associated with the expansion of a suppressive double-negative NKT cells and Foxp3<sup>+</sup> T<sub>Reg </sub>cells. The inventors also demonstrate herein
that pretreatment of adult mice with a glycolipid derived from <i>Helicobacter pylori </i>partially suppresses airway hyperreactivity and inhibits BAL inflammation in an ozone-exposure
model. Accordingly, provided herein are compositions and methods for the treatment and prevention of inflammatory diseases, such as asthma or autoimmune diseases, in a subject in need
thereof.</p>
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A novel compound (KS-513) isolated from Pseudolysimachion rotundum var. subintegrum, the composition comprising the same preventing or treating allergic disease, inflammatory disease, asthma or chronic obstructive pulmonary disease and the use thereof
(Fri, 20 Apr 2018)
<p id="p-0001"
num="0000">(1aS,1bS,2S,4S,5aR,6S,6aS)-1a-(hydroxymethyl)-4-methoxy-2-(((2S,3R,5S5,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)oxy)octahydrooxireno[2′,3′:4,5]cyclopenta[1,2-c]pyran-6-yl
4-hydroxybenzoate}, the isomer thereof, the pharmaceutically acceptable salt or solvates thereof, a composition comprising the same as an active ingredient for treating allergic disease, inflammatory
disease, asthma or chronic obstructive pulmonary disease (COPD) and the use thereof.</p>
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ISOLATED PEPTIDES AND FRAGMENTS THEREOF FROM FIBRINOGEN FOR USE AS DRUGS, PARTICUARLY IN SKIN INFLAMMATORY DISEASES
(Fri, 20 Apr 2018)
<p id="p-0001" num="0000">A present invention relates to isolated peptides obtained from human fibrinogen for their use as drug, particularly for the prevention and/or the treatment of
inflammatory skin diseases, more particularly acne. The present invention also relates to fragments of these polypeptides, nucleic acid molecules encoding them, expression vectors, host cells, a
pharmaceutical composition and a combination product containing them, and their use for treating and/or preventing inflammatory skin diseases, particularly acne.</p>
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N-ARYL AND N-HETEROARYL PIPERIDINE DERIVATIVES AS LIVER X RECEPTOR β AGONISTS, COMPOSITIONS, AND THEIR USE
(Fri, 20 Apr 2018)
Provided herein are certain substituted N-aryl and N-heteroaryl piperidine compounds of the formula (I) and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, L, R4, L1, Q, R5 and R 6 are
as defined. The said novel compounds, and pharmaceutically acceptable compositions comprising a compound thereof, may be useful as Liver X-β receptor(LXRβ) agonists, and may be useful for treating or
preventing pathologies related thereto. Such pathologies include, but are not limited to, inflammatory disease and diseases characterized by defects in cholesterol and lipid metabolism, such as
Alzheimer's disease.
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INHIBITORS OF ALPHA-AMINO-BETA-CARBOXYMUCONIC ACID SEMIALDEHYDE DECARBOXYLASE
(Fri, 20 Apr 2018)
The present disclosure discloses compounds capable of modulating the activity of α- amino-β-carboxymuconic acid semialdehyde decarboxylase (ACMSD), which are useful for the prevention and/or the
treatment of diseases and disorders associated with defects in NAD+ biosynthesis, e.g., metabolic disorders, neurodegenerative diseases, chronic inflammatory diseases, kidney diseases, and diseases
associated with ageing. The present application also discloses pharmaceutical compositions comprising said compounds and the use of such compounds as a medicament.
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N-ARYL AND N-HETEROARYL PIPERIDINE DERIVATIVES AS LIVER X RECEPTOR BETA AGONISTS, COMPOSITIONS, AND THEIR USE
(Fri, 20 Apr 2018)
In its many embodiments, the present invention provides certain substituted N-aryl and N-heteroaryl piperidine compounds of the Formula (I): (Formula (I)) and pharmaceutically acceptable salts
thereof, wherein R1, R2, R3, L, R4, L1,Q, R5 and R6 are as defined herein. The novel compounds of the invention, and pharmaceutically acceptable compositions comprising a compound thereof, may be
useful as Liver X-β receptor (LXRβ) agonists, and may be useful for treating or preventing pathologies related thereto. Such pathologies include, but are not limited to, inflammatory diseases and
diseases characterized by defects in cholesterol and lipid metabolism, such as Alzheimer's disease.
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ARYL AND HETEROARYL ETHER DERIVATIVES AS LIVER X RECEPTOR BETA AGONISTS
(Fri, 20 Apr 2018)
In its many embodiments, the present invention provides certain substituted aryl and heteroaryl ether compounds of the Formula (I): and pharmaceutically acceptable salts thereof, wherein X, R1, R2,
R3, L, R4, L1,Q, and R5 are as defined herein. The novel compounds of the invention, and pharmaceutically acceptable compositions comprising a compound thereof, are useful as Liver X-β receptor
(LXRβ) agonists, and may be useful for treating or preventing pathologies related thereto. Such pathologies include, but are not limited to, inflammatory diseases and diseases characterized by
defects in cholesterol and lipid metabolism, such as Alzheimer's disease.
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IMMUNOGLOBULIN SINGLE VARIABLE DOMAIN ANTIBODIES AGAINST OX40L, CONSTRUCTS AND THERAPEUTIC USE
(Thu, 19 Apr 2018)
The present invention relates to immunoglobulin single variable domain sequences that are directed against (as defined herein) OX40L, as well as to compounds or constructs, and in particular proteins
and polypeptides, that comprise or essentially consist of one or more such immunoglobulin single variable domain sequences. In particular these immunoglobulin single variable domain sequences can
block binding of OX40L to OX40. The immunoglobulin single variable domains, compounds and constructs can be used for prophylactic, therapeutic or diagnostic purposes, such as for the treatment of
inflammatory disease and/or disorder such as e.g. asthma, allergic asthma, chronic colitis, Crohn's disease, inflammatory bowel disease, and/or arthrosclerosis.
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COMPOUNDS AND COMPOSITIONS FOR TREATING LEISHMANIASIS AND METHODS OF DIAGNOSIS AND TREATING USING SAME
(Fri, 13 Apr 2018)
<p id="p-0001" num="0000">Compositions and methods of using these compositions that can include a targeting moiety and a therapeutic agent are described herein. These compositions can be used
for treating inflammatory diseases, such as parasitic diseases that result in cutaneous lesions. For example, and without limitation, such an parasitic disease can be leishmaniasis.</p>
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CRYSTAL FORMS OF IMMUNOMODULATORY DRUG POMALIDOMIDE AND CO-CRYSTAL WITH GENTISIC ACID
(Fri, 13 Apr 2018)
<p id="p-0001" num="0000">The present invention relates to novel solid crystal forms of Pomalidomide named Form B, Form M, Pomalidomide:Gentisic acid co-crystal and their preparation.
Advantageously, these solid forms are used in pharmaceutical compositions for the treatment and the prevention of multiple myeloma, of inflammatory diseases, of autoimmune diseases, of immune
diseases, of myelodysplastic syndrome, of myeloproliferative disorders, of anemia, of scleroderma, amyloidosis or of other diseases associated with unwanted angiogenesis.</p>
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TRICYCLIC COMPOUND AND JAK INHIBITOR
(Fri, 13 Apr 2018)
<p id="p-0001" num="0000">Novel tricyclic compounds which have JAK inhibitory activities are useful for prevention, treatment or improvement of autoimmune diseases, inflammatory diseases and
allergic diseases are provided.</p> <p id="p-0002" num="0000">Novel tricyclic compound represented by the formula (I), the formula (II) or the formula (III) (wherein: each of
A<sup>1</sup>, A<sup>2 </sup>and A<sup>3 </sup>is a cyclohexane-1,4-diyl group or the like; each of L<sup>1</sup>, L<sup>2 </sup>and
L<sup>3 </sup>is a methylene group or the like; each of X<sup>1 </sup>and X<sup>3 </sup>is 0 or NH; each of R<sup>1 </sup>and R<sup>3
</sup>is a cyano C<sub>1-6 </sub>haloalkyl group or the like; and R<sup>2 </sup>is an aromatic heterocyclic group), a tautomer or pharmaceutically acceptable salt of the
compound or a solvate thereof.</p> <p id="p-0003" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="113.79mm" wi="58.59mm"
file="US20180099966A1-20180412-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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BIFUNCTIONAL STAPLED POLYPEPTIDES AND USES THEREOF
(Fri, 13 Apr 2018)
<p id="p-0001" num="0000">The invention relates to bifunctional stapled or stiched peptides comprising a targeting domain, a linker moiety, and an effector domain, that can be used to tether,
or to bring into close proximity, at least two cellular entities (e.g., proteins). Certain aspects relate to bifunctional stapled or stiched peptides that bind to an effector biomolecule through the
effector domain and bind to a target biomolecule through the targeting domain. Polypeptides and/or polypeptide complexes that are tethered by the bifunctional stapled or stiched peptides of the
invention, where the effector polypeptide bound to the effector domain of the bifunctional stapled or stiched peptide modifies or alters the target polypeptide bound to the targeting domain of the
bifunctional peptide. Usesses of the inventive bifunctional stapled or stiched peptides including methods for treatment of disease (e.g., cancer, inflammatory diseases) are also provided.</p>
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COMPOUNDS AND COMPOSITIONS FOR TREATING LEISHMANIASIS AND METHODS OF DIAGNOSIS AND TREATING USING SAME
(Fri, 13 Apr 2018)
Compositions and methods of using these compositions that can include a targeting moiety and a therapeutic agent are described herein. These compositions can be used for treating inflammatory
diseases, such as parasitic diseases that result in cutaneous lesions. For example, and without limitation, such an parasitic disease can be leishmaniasis.
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TRICYCLIC INHIBITORS OF POLY(ADP-RIBOSE)POLYMERASE
(Fri, 06 Apr 2018)
<p id="p-0001" num="0000">The invention provides for compositions comprising phosphorous containing tricyclic compounds, including phthalazin-1(2H)-one derivatives. The compounds are potent
inhibitors of the enzyme poly(ADP-ribose)polymerase (PARP), particularly PARP-1 and potentially PARP-2. The also show good cellular activity in inhibiting poly(ADP-ribose) oligomer formation. The
compounds may be useful as mono-therapy or in combination with other therapeutic agents in the treatment conditions where PARP is implicated, such as cancer, inflammatory diseases and ischemic
conditions. Thus, also provided are methods for the treatment of a condition where PARP is implicated comprising administering to an effective amount of a compound of the invention to an individual
in need thereof.</p>
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RETINOID DERIVATIVES WITH ANTITUMOR ACTIVITY
(Fri, 06 Apr 2018)
The present invention relates to compounds of formula (I) and to pharmaceutical compositions containing them, wherein meanings of the substituents are indicated in the description. Such compounds for
use in the treatment of cancer and other diseases related to altered angiogenesis, such as arthritic pathology, diabetic retinopathy, psoriasis and chronic inflammatory disease, are also within the
scope of the present invention.
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SUBSTITUTED N-(1H-INDAZOL-4-YL)IMIDAZO[1,2-a]PYRIDINE-3-CARBOXAMIDE COMPOUNDS AS TYPE III RECEPTOR TYROSINE KINASE INHIBITORS
(Fri, 06 Apr 2018)
[007801 Compounds of Formula I: and pharmaceutically acceptable salts thereof in which R', R2, R, R4, R5 and R6 have the meanings given in the specification, are inhibitors of cFMS and are useful in
the treatment of fibrosis, bone-related diseases, cancer, autoimmune disorders, inflammatory diseases, cardiovascular diseases, pain and burns in a mammal.
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RETINOID DERIVATIVES WITH ANTITUMOR ACTIVITY
(Thu, 05 Apr 2018)
The present invention relates to new compounds of formula (I) and to pharmaceutical compositions containing them: The use of such compounds for the treatment of cancer and other diseases related to
altered angiogenesis, such as arthritic pathology, diabetic retinopathy, psoriasis and chronic inflammatory disease, is also within the scope of the present invention.
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BENZIMIDAZOLE DERIVATIVES AND THEIR USE AS PHOSPHATIDYLINOSITOL 3-KINASE INHIBITORS
(Fri, 30 Mar 2018)
The present application provides the compounds of formula I or pharmaceutically acceptable salts, isomers, tautomer, or a mixture thereof, wherein t, R1, R2, R3, R4, and R6 are as described herein.
The compounds of formula I selectively inhibit the activities of PI3K isoforms and are useful in therapeutic treatments, in particular in the treatment of inflammatory diseases and cancer.
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NOVEL COMPOUND USEFUL FOR THE TREATEMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES
(Fri, 23 Mar 2018)
<p id="p-0001" num="0000">A pyrazolopyridine compound according to Formula I, able to inhibit JAK is disclosed, as well as pharmaceutically acceptable salts, a solvate thereof, solvates of the
pharmaceutically acceptable salts and biologically active metabolites thereof. The compound may be prepared as a pharmaceutical composition, and may be used for the treatment or prophylaxis of a
variety of conditions in mammals including humans, and particularly, such conditions as may be associated with aberrant JAK activity, including by way of non-limiting example, allergy, inflammatory
conditions, autoimmune diseases, proliferative diseases, transplant rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with
hypersecretion of IL6.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="53.93mm" wi="69.85mm"
file="US20180078547A1-20180322-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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Fumarate Analogs and Uses Thereof
(Fri, 16 Mar 2018)
<p id="p-0001" num="0000">Aspects of the present disclosure include compounds that find use for the treatment of a variety of autoimmune and inflammatory diseases and disorders. Embodiments of
the present disclosure also relate to pharmaceutical compositions that include these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for
preparing these compounds and intermediates useful in these processes.</p>
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USE OF RECOMBINANT LYMPHOCYTE ACTIVATION GENE-3
(Fri, 16 Mar 2018)
A method for classifying patients at risk for cardiovascular disease, other chronic inflammatory diseases, cardiovascular and/or non-cardiovascular morbidity and mortality based on a risk assessment
for lymphocyte activation gene 3 (LAG3) protein deficiency, and for mediating the risk using recombinant lymphocyte activation gene-3 or LAG3 mimetic as a companion therapeutic alone or in
combination with a statin and/or an anti-hyperlipidemic drug, The risk assessment is two-prong, beginning with a qualitative determination whether a subject has of is predisposed to abnormal
expression of inflammasomes, heightened risk for inflammation and/or to dysfunctional HDL, followed, by a quantitative assay or genetic screen for a polymorphism that occurs in the coding sequence of
the LAG3 gene. Given positive indication, recombinant LAG3 and/or LAG3 mimetic is used alone or in combination with the therapeutic use of a cholesterol mediating, drug for treatment.
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SITE SPECIFIC CURCUMIN-POLYMER MOLECULAR COMPLEXES AND METHODS OF TREATING COLON DISEASES AND INFLAMMATION
(Fri, 09 Mar 2018)
<p id="p-0001" num="0000">Methods and materials relating to a medicament preparation comprising a curcuminoid component, such as curcumin, and a polymer component having a backbone comprising
polymethacrylate or methyl methacrylate provided as a curcuminoid-polymer complex, which enhances the solubility, stability and bioavailability of the curcumin component and are useful for the
treatment of various inflammatory diseases and conditions when delivered to the gastro-intestinal tract, including sepsis, mucositis, gastritis, infections, inflammatory bowel disease and cancers of
GIT. The curcumin-polymer complex inhibiting the activation of TLR receptors and thereby reduce the release of inflammatory cytokines, such that the curcumin-polymer complexes are more potent than
free curcumin in antagonizing on the activation of TLR4.</p>
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IMIDAZOLE DERIVATIVES AND THEIR USE IN THE TREATMENT OF AUTOIMMUNE OR INFLAMMATORY DISEASES OR CANCERS
(Fri, 09 Mar 2018)
Compounds of formula (I) and salts thereof: Formula (I) wherein R1, R2, R3 and a are as defined herein. Compounds of formula (I) and salts thereof have been found to inhibit the binding of the BET
family of bromodomain containing proteins to, for example, acetylated lysine residues and thus may have use in therapy, for example in the treatment of autoimmune and inflammatory diseases, such as
rheumatoid arthritis; and cancers.
>> Read More

IMIDAZOLE DERIVATIVES AND THEIR USE IN THE TREATMENT OF AUTOIMMUNE OR INFLAMMATORY DISEASES OR CANCERS
(Fri, 09 Mar 2018)
Compounds of formula (I) and salts thereof: wherein R1, R2, R3, a, X1, X2, X3, X4, and X5 are as defined hereinbefore. Compounds of formula (I) and salts thereof have been found to inhibit the
binding of the BET family of bromodomain containing proteins to, for example, acetylated lysine residues and thus may have use in therapy, for example in the treatment of autoimmune and inflammatory
diseases, such as rheumatoid arthritis; and cancers.
>> Read More

Purinone compounds as kinase inhibitors
(Fri, 09 Mar 2018)
Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. In addition, reversible inhibitors of Btk are also
described. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the
treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.
>> Read More

LANTHIONINE SYNTHETASE C-LIKE 2-BASED THERAPEUTICS
(Fri, 02 Mar 2018)
<p id="p-0001" num="0000">Provided are compounds that target the lanthionine synthetase C-like protein 2 pathway. The compounds can be used to treat a number of conditions, including infectious
disease, autoimmune disease, diabetes, and a chronic inflammatory disease.</p>
>> Read More

PRODRUGS ACTIVATED BY REACTIVE OXYGEN SPECIES FOR USE IN THE TREATMENT OF INFLAMMATORY DISEASES AND CANCER
(Fri, 02 Mar 2018)
Prodrugs activated predominantly or exclusively in inflammatory tissue, more particularly prodrugs of methotrexate and derivatives thereof, which are selectively activated by Reactive Oxygen Species
(ROS) in inflammatory tissues associated with cancer and inflammatory diseases, as well as method for preparing said prodrugs.
>> Read More

PRODRUGS ACTIVATED BY REACTIVE OXYGEN SPECIES FOR USE IN THE TREATMENT OF INFLAMMATORY DISEASES AND CANCER
(Fri, 02 Mar 2018)
Prodrugs activated predominantly or exclusively in inflammatory tissue, more particularly prodrugs of methotrexate and derivatives thereof, which are selectively activated by Reactive Oxygen Species
(ROS) in inflammatory tissues associated with cancer and inflammatory diseases, as well as method for preparing said prodrugs.
>> Read More

NOVEL HETEROCYCLIC COMPOUNDS AND USE THEREOF IN MEDICINE AND IN COSMETICS
(Fri, 23 Feb 2018)
<p id="p-0001" num="0000">The invention relates to novel heterocyclic compounds of general formula (I), as well as their pharmaceutically acceptable salts, and their enantiomers. The invention
also relates to the use thereof as a medicinal product, preferably in the prevention and/or treatment of inflammatory diseases with a neurogenic component or use thereof as a cosmetic. The compounds
of the present invention act as antagonists of the CGRP-R receptor.</p>
>> Read More

Derivatives of 1-[(cyclopentyl or 2-pyrrolidinyl)carbonylaminomethyl]-4-(1,3-Thiazol-5-yl) benzene which are Useful for the Treatment of Proliferative, Autoimmune or Inflammatory Diseases
(Fri, 23 Feb 2018)
<p id="p-0001" num="0000">There is provided novel small molecule E3 ubiquitin ligase protein binding ligand compounds, having utility in PROteolysis Targeted Chimeras (PROTACs), as well as
processes for the preparation thereof, and use in medicine. There is particularly provided PROTACs which bind to a protein within the bromo- and Extra-terminal (BET) family of proteins, and
especially to PROTACs including novel small molecule E3 ubiquitin ligase protein binding ligand compounds which selectively induce degradation of the BRD4 protein within the bromodomain of the BET
family of proteins.</p>
>> Read More

KINASE INHIBITORS
(Fri, 16 Feb 2018)
<p id="p-0001" num="0000">There are provided compounds of formula I,</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001"
he="48.60mm" wi="76.03mm" file="US20180044288A1-20180215-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003"
num="0000">wherein R<sup>1A </sup>to R<sup>1E</sup>, R<sup>2 </sup>to R<sup>5</sup>, L and X<sup>1 </sup>to X<sup>3
</sup>have meanings given in the description, which compounds have antiinflammatory activity (e.g. through inhibition of one or more of members of: the family of p38 mitogen-activated protein
kinase enzymes; Syk kinase; and members of the Src family of tyrosine kinases) and have use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases,
including inflammatory diseases of the lung, eye and intestines.</p>
>> Read More

Pyridinone and pyridazinone derivatives
(Fri, 16 Feb 2018)
The present invention provides for compounds of formula (I) wherein J is a group of formula Ha or Ilb: A1 , A2 , A', A4 , J, and X3 have any of the values defined therefor in the specification, and
pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, diabetes, obesity, cancer, and AIDS. Also provided
are pharmaceutical compositions comprising one or more compounds of formula I.
>> Read More

SPECIFICALLY meso-SUBSTITUTED PORPHYRINS AND CHLORINS FOR PHOTODYNAMIC THERAPY
(Fri, 09 Feb 2018)
<p id="p-0001" num="0000">Biologically active compounds that can be used as photosensitizers for diagnostic and therapeutic applications, particularly for PDT of cancer, infections and other
hyperproliferative diseases, fluorescence diagnosis and PDT treatment of a non-tumorous indication such as arthritis, inflammatory diseases, viral or bacterial infections, dermatological,
opthamological or urological disorders are provided as well as providing methods to obtain them in pharmaceutical quality. One embodiment consists of a method to synthesize a porphyrin with a defined
arrangement of meso-substituents and then converting this porphyrin system to a chlorin system by dihydroxylation or reduction, and if more than one isomer is formed separate them by chromatography
either on normal or reversed phase silica. In another embodiment the substituents on the porphyrin are selected to direct the reduction or dihydroxylation to the chlorin so that a certain isomer is
selectively formed. Another embodiment is to provide amphiphilic compounds with a higher membrane affinity and increased PDT-efficacy. In other embodiments the nucleophilic substitution on
pentafluorophenyl-substituted tetrapyrroles is used to obtain compounds with a high PDT-efficacy. In another embodiment substituents are identified that via their steric and/or electronic influence
direct the dihydroxylation or reduction with diimine so that one isomer is favored. Another embodiment consists of formulating the desired tetrapyrrole photosensitizer into a pharmaceutical
formulation to be injected into the body avoiding undesirable effects like solubility problems or delayed pharmacokinetics of the tetrapyrrole systems.</p>
>> Read More

SUBSTITUTED PYRIMIDINE COMPOUNDS AS PHOSPHATIDYLINOSITOL 3-KINASE DELTA INHIBITOR AND USE THEREOF
(Fri, 09 Feb 2018)
<p id="p-0001" num="0000">The present invention belongs to the field of medicinal chemistry, and relates to substituted pyrimidine compounds as phosphatidylinositol 3-kinase (PI3K) δ inhibitor
and a use thereof. In particular, the present invention provides a compound as shown by formula I or an isomer, pharmaceutically acceptable salt, solvate or prodrug thereof, the preparation methods
of same and pharmaceutical compositions containing these compounds and a use of these compounds or compositions for treating cancer, hyperblastosis diseases or inflammatory diseases. The compounds of
the present invention have a good inhibiting activity on PI3Kδ and have a high selectivity. It is hoped that these will be therapeutic agents for cancer, hyperblastosis diseases or inflammatory
diseases.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="39.03mm" wi="66.46mm" file="US20180037576A1-20180208-C00001.TIF"
alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
>> Read More

PURINONE COMPOUNDS AS KINASE INHIBITORS
(Fri, 09 Feb 2018)
<p id="p-0001" num="0000">Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. In addition, reversible
inhibitors of Btk are also described. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other
therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.</p>
>> Read More

LIPID-SUBSTITUTED AMINO 1,2-AND 1,3-DIOL COMPOUNDS AS MODULATORS OF TLR2 DIMERIZATION
(Fri, 09 Feb 2018)
The present invention relates to lipid-substituted amino 1,2- and 1,3-diol compounds, pharmaceutical compositions comprising such compounds, and use of such compounds in methods of treatment or in
medicaments for treatment of inflammatory diseases and certain neurological disorders that are related to inflammatory signaling processes, including but not limited to misfolded proteins.
>> Read More

Novel Formulations of a Bruton's Tyrosine Kinase Inhibitor
(Fri, 02 Feb 2018)
<p id="p-0001" num="0000">Described herein is the Bruton's tyrosine kinase (Btk) inhibitor 1-((R)-3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one,
including novel pharmaceutical formulations thereof. Also disclosed are pharmaceutical compositions that include the Btk inhibitor, as well as methods of using the Btk inhibitor, alone or in
combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or
conditions.</p>
>> Read More

INHIBITORS OF BRUTON'S TYROSINE KINASE
(Fri, 02 Feb 2018)
<p id="p-0001" num="0000">Disclosed herein are reversible and irreversible inhibitors of Bruton's tyrosine kinase (Btk). Also disclosed are pharmaceutical compositions that include the
compounds. Methods of using the Btk inhibitors are describeded, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or
conditions, cancer, including lymphoma, and inflammatory diseases or conditions.</p>
>> Read More

MODIFICATIONS OF THERAPEUTIC AGENTS FOR ENHANCED DELIVERY TO TARGET SITES
(Fri, 02 Feb 2018)
<p id="p-0001" num="0000">Compositions of a modulator of cell metabolism, typically targeting cellular glycolysis, preferably with a targeting moiety, attached directly or indirectly to the
inhibitor, or to a nanoparticle or other delivery vehicle thereof, and methods of use for treating cancer, proliferative disorders, neurodegenerative diseases, autoimmune disorders, or inflammatory
diseases are provided. Pharmaceutical compositions including the targeted modulator and a pharmaceutically acceptable carrier are also provided. The pharmaceutical compositions can be administered to
a subject in need thereof in an effective amount to reduce one or symptoms of the cancer, proliferative disorders, neurodegenerative diseases, autoimmune disorders, or inflammatory diseases alone or
prior to or in conjunction with a further therapy such as radiotherapy.</p>
>> Read More

SUBSTITUTED THIAZOLO-PYRIDINE COMPOUNDS AS MALT1 INHIBITORS
(Fri, 02 Feb 2018)
Disclosed are compounds of the general formula (I), wherein R1-R3 are as defined herein, for use as MALT1 inhibitors in the treatment of autoimmune and inflammatory diseases or disorders. Methods of
synthesizing the compounds are also disclosed. Also disclosed are pharmaceutical compositions containing a compound of the invention and a method of treating a patient for an autoimmune or an
inflammatory disease or disorder, for example, a cancer, by administering a compound of the invention.
>> Read More

OPTIMISED COMBINATION THERAPY AND USE THEREOF TO TREAT CANCER AND AUTOIMMUNE DISEASE
(Thu, 25 Jan 2018)
Provided is a series of new poly-fluorosubstituted pyrazolopyrimidine compounds or salts. The compounds are Bruton's tyrosine kinase (BTK) inhibitors. The compounds have better kinase inhibition
selectivity and pharmokinetic properties. Also provided is a preparation method for the compounds. Also provided is a combination therapy including the compounds in combination with another targeted
drug composition or another drug. The optimised combination therapy has a cooperative effect, inhibits the existence of a tumour better than a single targeted drug, and causes certain tumours to
completely disappear. The optimised combination therapy treats drug resistance and cancer recurrence of a tumour better than a single targeted drug, and the treatment cycle is shorter. The present
invention also relates to a combined compound and a pharmaceutical preparation wherein said combined compound acts as an active ingredient, said pharmaceutical preparation being safer at a lower
dosage and having a cooperative effect efficacy. Also provided is a method of using the compounds and a preparation thereof to treat and inhibit an autoimmune disease or illness, a heterogeneous
autoimmune disease or illness, an inflammatory disease, a cancer or an illness.
>> Read More

SITE SPECIFIC DOSING OF A BTK INHIBITOR
(Fri, 19 Jan 2018)
<p id="p-0001" num="0000">Disclosed herein are formulations and methods of site specific administration of Compound (I) or a pharmaceutically acceptable salt thereof. Compound (I) is a potent
BTK inhibitor and hence can be useful for the treatment of diseases such as cancer, autoimmune, and inflammatory diseases.</p>
>> Read More

PYRIMIDINONE DERIVATIVES AND USES THEREOF TO NEUTRALIZE THE BIOLOGICAL ACTIVITY OF CHEMOKINES
(Fri, 19 Jan 2018)
A subject of the present invention is a compound having the general formula (I) a pharmaceutically acceptable salt thereof or a tautomeric form thereof, wherein A, B3, B4, B5, Y, X, B1 and B2 are as
defined in any one of claims 1 to 10. Another subject of the invention is the compound as defined above for use as a medicament, in particular for preventing and/or treating inflammation and
inflammatory diseases, immune and auto-immune diseases, pain related diseases, genetic diseases and/or cancer.
>> Read More

Heterocyclic compounds and use thereof
(Fri, 12 Jan 2018)
<p id="p-0001" num="0000">Heterocyclic compounds of Formula (I) shown herein. Also disclosed are pharmaceutical compositions containing the heterocyclic compounds and methods of using the
heterocyclic compounds to mobilize hematopoietic stem cells and endothelial progenitor cells into the peripheral circulation. Further provided are methods for treating tissue injury, cancer,
inflammatory disease, and autoimmune disease with the heterocyclic compounds.</p>
>> Read More

2-oxo-1,2-dihydrobenzo[cd]indole compound and use thereof
(Fri, 12 Jan 2018)
<p id="p-0001" num="0000">The present invention relates to the technical field of medicinal chemistry, and in particular discloses a 2-oxo-1,2-dihydrobenzo[cd]indole compound and use thereof.
The compound and pharmaceutically acceptable salt, isomer, racemate, prodrug, co-crystallized complex, hydrate, and solvate thereof can effectively inhibit the BET bromodomain receptor, and can be
used for preparing a medicine for treating cancers, cell proliferative disorders, inflammatory diseases, and autoimmune disorders, sepsis, and viral infections.</p>
>> Read More

IMIDAZO[1,2-A]PYRIDINE DERIVATIVES, METHODS FOR PREPARING THE SAME AND USE THEREOF
(Fri, 12 Jan 2018)
The present disclosure relates to novel imidazo[1,2-a]pyridine derivatives, and more particularly to imidazo[1,2-a]pyridine derivatives having an excellent activity of inhibiting gastric acid
secretion, methods for preparing the same, and the use thereof. The imidazo[1,2-a]pyridine derivatives according to the present disclosure have gastric acid secretion inhibitory activity, and thus
may be effectively used for the prevention or treatment of gastrointestinal inflammatory diseases or gastric acid-related diseases.
>> Read More

SUBSTITUTED PYRIMIDINE COMPOUNDS AS PHOSPHATIDYLINOSITOL 3-KINASE DELTA INHIBITOR AND USE THEREOF
(Thu, 11 Jan 2018)
The present invention belongs to the field of medicinal chemistry, and relates to substituted pyrimidine compounds as phosphatidylinositol 3-kinase (PI3K) ´ inhibitor and a use thereof. In
particular, the present invention provides a compound as shown by formula I or an isomer, pharmaceutically acceptable salt, solvate or prodrug thereof, the preparation methods of same and
pharmaceutical compositions containing these compounds and a use of these compounds or compositions for treating cancer, hyperblastosis diseases or inflammatory diseases. The compounds of the present
invention have a good inhibiting activity on PI3K´ and have a high selectivity. It is hoped that these will be therapeutic agents for cancer, hyperblastosis diseases or inflammatory diseases.
>> Read More

BICYCLIC COMPOUND
(Fri, 05 Jan 2018)
<p id="p-0001" num="0000">Provided is a bicyclic compound having an acetyl-CoA carboxylase inhibitory action. A compound represented by the formula:</p> <p id="p-0002"
num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="28.02mm" wi="67.90mm" file="US20180002322A1-20180104-C00001.TIF" alt="embedded image" img-content="chem"
img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">wherein each symbol is as described in the DESCRIPTION, or a salt thereof has an acetyl-CoA carboxylase inhibitory
action, is useful for the prophylaxis or treatment of cancer, inflammatory diseases and the like, and has superior efficacy.</p>
>> Read More

NOVEL COMPOUND USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES
(Fri, 05 Jan 2018)
<p id="p-0001" num="0000">A novel compound able to inhibit JAK is disclosed, this compound may be prepared as a pharmaceutical composition, and may be used for the prevention and treatment of a
variety of conditions in mammals including humans, including by way of non-limiting example, inflammatory conditions, autoimmune diseases, proliferative diseases, transplantation rejection, diseases
involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6.</p>
>> Read More

4,6-DIAMINOQUINAZOLINES AS COT MODULATORS AND METHODS OF USE THEREOF
(Fri, 05 Jan 2018)
The invention relates to 4,6-diaminoquinazoline derivatives of formula I which are modulators of the Cot (cancer Osaka thyroid) kinase, also known as MAP3K8, EST or Tlp-2, and their use for treating
e.g. cancer, diabetes and inflammatory diseases.
>> Read More

Oxidized Lipids and Methods of Use Thereof
(Fri, 29 Dec 2017)
<p id="p-0001" num="0000">The present invention is directed to oxidized lipids and pharmaceutical compositions comprising the same. The present invention is also directed to methods of making
an oxidized lipid of the invention and to methods of treating or preventing fibrosis or inflammatory diseases or disorders comprising an oxidized lipid of the invention.</p>
>> Read More

Cyclic Compounds and Uses Thereof
(Fri, 29 Dec 2017)
<p id="p-0001" num="0000">The invention generally relates to substituted benzothiophenyl, substituted benzothiazolyl, substituted indolyl and substituted benzoimidazolyl compounds and, more
particularly, to a compound represented by Structural Formula I: or a pharmaceutically acceptable salt thereof, wherein the variables are as defined and described herein. The invention also includes
the synthesis and use of a compound of Structural Formula I, or a pharmaceutically acceptable salt or composition thereof, e.g., in the treatment of a disease or disorder selected from cancer (e.g.,
lymphoma, such as mantle cell lymphoma), a neurodegenerative disease, inflammatory diseases or an autoimmune system disease (e.g., a T-Cell mediated autoimmune disesase).</p> <p id="p-0002"
num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="27.86mm" wi="64.43mm" file="US20170369470A1-20171228-C00001.TIF" alt="embedded image" img-content="chem"
img-format="tif"/> </chemistry> </p>
>> Read More

NON-CATALYTIC SUBSTRATE-SELECTIVE P38α-SPECIFIC MAPK INHIBITORS WITH ENDOTHELIAL-STABILIZING AND ANTI-INFLAMMATORY ACTIVITY, AND METHODS OF USE THEREOF
(Fri, 29 Dec 2017)
Compounds that inhibit p38α MAPK protein, and methods of using the same, are provided for treating or preventing diseases such as cancer or inflammatory diseases.
>> Read More

DRUG DELIVERY CONJUGATES CONTAINING UNNATURAL AMINO ACIDS AND METHODS FOR USING
(Fri, 22 Dec 2017)
<p id="p-0001" num="0000">Described herein are drug delivery conjugates for targeted therapy. In particular, described herein are drug delivery conjugates that include polyvalent linkers
comprising one or more unnatural amino acids that are useful for treating cancers and inflammatory diseases.</p>
>> Read More

INHIBITORS OF ALPHA-AMINO-BETA-CARBOXYMUCONIC ACID SEMIALDEHYDE DECARBOXYLASE
(Fri, 22 Dec 2017)
<p id="p-0001" num="0000">The present disclosure discloses compounds capable of modulating the activity of α-amino-β-carboxymuconic acid semialdehyde decarboxylase (ACMSD), which are useful for
the prevention and/or the treatment of diseases and disorders associated with defects in NAD<sup>+</sup> biosynthesis, e.g., metabolic disorders, neurodegenerative diseases, chronic
inflammatory diseases, kidney diseases, and diseases associated with ageing. The present application also discloses pharmaceutical compositions comprising said compounds and the use of such compounds
as a medicament.</p>
>> Read More

4,6-SUBSTITUTED-PYRAZOLO[1,5-a]PYRAZINES AS JANUS KINASE INHIBITORS
(Fri, 22 Dec 2017)
<p id="p-0001" num="0000">Compounds of Formula I: and stereoisomers and pharmaceutically acceptable salts and solvates thereof in which R<sup>1</sup>, R<sup>2</sup>,
R<sup>3 </sup>and R<sup>4 </sup>have the meanings given in the specification, are inhibitors of one or more JAK kinases and are useful in the treatment of JAK
kinase-associated diseases and disorders, such as autoimmune diseases, inflammatory diseases, rejection of transplanted organs, tissues and cells, as well as hematologic disorders and malignancies
and their co-morbidities.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="48.01mm" wi="59.10mm"
file="US20170362240A1-20171221-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
>> Read More

PHARMACEUTICAL COMPOSITIONS AND THEIR USE FOR TREATMENT OF CANCER AND AUTOIMMUNE DISEASES
(Fri, 22 Dec 2017)
Described herein are combination therapies for cancer (such as lymphoid malignancies) and immune diseases (such as autoimmune diseases and inflammatory diseases). The therapies comprise the combined
use of inhibitors of BTK, mTOR kinase, and Bcl-2 or their signaling pathways, and immunomodulatory drugs. Also described are pharmaceutical compositions and kits comprising these inhibitors.
>> Read More

Novel 5-HT2 antagonists
(Fri, 22 Dec 2017)
The present invention relates to 1-amidino-3-aryl-2-pyrazoline derivatives of the general formula I The invention specifically relates to such derivatives which exhibit antagonizing activity towards
serotonin 5-HT<sb>2B</sb> receptors. The present invention also relates to use of said compounds as a medicament and for the treatment of fibrosis, cardiovascular diseases, pain, IBD, and
other inflammatory diseases, as well as pharmaceutical compositions comprising one or more of said compounds and methods of treatment.
>> Read More

IL-18 binding molecules
(Fri, 22 Dec 2017)
IL-18 participates in both innate and acquired immunity. The bioactivity of IL-18 is negatively regulated by the IL-18 binding protein (IL18BP), a naturally occurring and highly specific inhibitor.
This soluble protein forms a complex with free IL-1 8 preventing its interaction with the IL-18 receptor, thus neutralizing and inhibiting its biological activity. The present invention discloses
binding molecules, in particular antibodies or fragments thereof, which bind IL-18 and do not bind IL-18 bound to IL-18BP (IL-18/IL-18BP complex). Apart from its physiological role, IL-18 has been
shown to mediate a variety of autoimmune and inflammatory diseases. The binding molecules of the inventions may be used as therapeutic molecules for treating IL-18-related autoimmune and inflammatory
diseases or as diagnostic tools for characterizing, detecting and/or measuring IL-18 not bound to IL-18BP as component of the total IL-18 pool.
>> Read More

(5R)-5-[3-[(3S)-4-(4-CHLORO-3-METHOXY-5-METHYL-PHENYL)-3-METHYL-PIPERAZIN-1-YL]- 3-OXO-PROPYL]-5-METHYL-IMIDAZOLIDINE-2,4-DIONE AS ADAMTS 4 AND 5 INHIBITOR FOR TREATING E.G. OSTEOARTHRITIS
(Fri, 15 Dec 2017)
The present invention discloses (5R)-5-[3-[(3S)-4-(4-chloro-3-methoxy-5-methyl-phenyl)-3-methyl-piperazin-l-yl]-3-oxo-propyl]-5-methyl-imidazolidine-2,4-dione according to Formula (I). The present
invention relates to the compound of formula (I) inhibiting ADAMTS 4 and 5 for the prophylaxis or treatment of inflammatory diseases or diseases involving degradation of cartilage or disruption of
cartilage homeostasis, such as e.g. osteoarthritis.
>> Read More

5-[3-[PIPERIDIN-1-YL]-3-OXO-PROPYL]-IMIDAZOLIDINE-2,4-DIONE DERIVATIVES AS ADAMTS 4 AND 5 INHIBITORS FOR TREATING E.G. OSTEOARTHRITIS
(Fri, 15 Dec 2017)
The present invention discloses 5-[3-[piperazin-l-yl]-3-oxo-propyl]-imidazolidine-2,4-dione derivatives according to Formula (I), wherein R1, R2, R3a, R3b, R6a, R6b, the subscript n and Cy are as
defined herein. The present invention relates to compounds inhibiting ADAMTS 4 and 5 for the prophylaxis or treatment of inflammatory diseases or diseases involving degradation of cartilage or
disruption of cartilage homeostasis, such as e.g. osteoarthritis.
>> Read More

5-[3-[PIPERAZIN-1-YL]-3-OXO-PROPYL]-IMIDAZOLIDINE-2,4-DIONE DERIVATIVES AS ADAMTS 4 AND 5 INHIBITORS FOR TREATING E.G. OSTEOARTHRITIS
(Fri, 15 Dec 2017)
The present invention discloses 5-[3-[piperazin-l-yl]-3-oxo-propyl]-imidazolidine-2,4-dione derivatives according to Formula (I), wherein R1, R2, R3a, R3b, R6a, R6b, the subscript n and Cy are as
defined herein. The present invention relates to compounds inhibiting ADAMTS 4 and 5 for the prophylaxis or treatment of inflammatory diseases or diseases involving degradation of cartilage or
disruption of cartilage homeostasis, such as e.g. osteoarthritis.
>> Read More

SERINE/THREONINE KINASE INHIBITORS
(Fri, 08 Dec 2017)
<p id="p-0001" num="0000">Compounds of Formula I or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof are provided, which are useful for the treatment of hyperproliferative,
pain and inflammatory diseases. Methods of using compounds of Formula I or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof, for in vitro, in situ, and in vivo diagnosis,
prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001"
num="00001"> <img id="EMI-C00001" he="28.79mm" wi="61.30mm" file="US20170348310A1-20171207-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry>
</p>
>> Read More

INHIBITORS OF INTERLEUKIN-1 RECEPTOR-ASSOCIATED KINASE
(Fri, 01 Dec 2017)
Disclosed herein are inhibitors of IRAK protein kinase. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the IRAK inhibitors are described, alone or in
combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or
conditions.
>> Read More

INHIBITORS OF INTERLEUKIN-1 RECEPTOR-ASSOCIATED KINASE
(Fri, 01 Dec 2017)
Disclosed herein are inhibitors of IRAK protein kinase of formula (I). Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the IRAK inhibitors are described,
alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory
diseases or conditions.
>> Read More

INHIBITORS OF INTERLEUKIN-1 RECEPTOR-ASSOCIATED KINASE
(Fri, 01 Dec 2017)
Disclosed herein are inhibitors of IRAK protein kinase of formula (I). Also disclosed are pharmaceutical compositions that include the compounds of formula (I). Methods of using the IRAK inhibitors
are described, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and
inflammatory diseases or conditions. Formula (I)
>> Read More

JAK AND HDAC DUAL-INHIBITOR COMPOUNDS
(Fri, 17 Nov 2017)
The present disclosure described provides novel dual inhibition compounds that specifically target the JAK-STAT and HDAC pathways, two distinct cellular pathways that are useful in the treatment of
various diseases and disorders. In certain aspects, the compounds described herein are useful in the treatment of cellular proliferative and inflammatory diseases or disorders, such as graft vs. host
disease. In particular embodiments, the compounds described herein inhibit JAK2 and HDAC6.
>> Read More

USE OF RECOMBINANT LYMPHOCYTE ACTIVATION GENE-3 AS A COMPANION THERAPEUTIC FOR PATIENTS AT RISK FOR CARDIOVASCULAR DISEASE AND OTHER CHRONIC INFLAMMATORY DISEASES
(Fri, 03 Nov 2017)
<p id="p-0001" num="0000">A method for classifying patients at risk for cardiovascular disease, other chronic inflammatory diseases, cardiovascular and/or non-cardiovascular morbidity and
mortality based on a risk assessment for lymphocyte activation gene 3 (LAG3) protein deficiency, and for mediating the risk using recombinant lymphocyte activation gene-3 or LAG3 mimetic as a
companion therapeutic alone or in combination with a statin and/or an anti-hyperlipidemic drug. The risk assessment is two-prong, beginning with a qualitative determination whether a subject has or
is predisposed to abnormal expression of inflammasomes, heightened risk for inflammation and/or to dysfunctional HDL, followed by a quantitative assay or genetic screen for a polymorphism that occurs
in the coding sequence of the LAG3 gene. Given positive indication, recombinant LAG3 and/or LAG3 mimetic is used alone or in combination with the therapeutic use of a cholesterol mediating drug for
treatment.</p>
>> Read More

1-PYRAZOLYL-3-(4-((2-ANILINOPYRIMIDIN-4 -YL) OXY) NAPTHTHALEN-1 - YL) UREAS AS P38 MAP KNASE INHIBITORS
(Fri, 03 Nov 2017)
<p id="p-0001" num="0000">There are provided compounds of formula (I) which are inhibitors of the family of p38 mitogen-activated protein kinase enzymes, and to their use in therapy, including
in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, such as asthma and COPD.</p>
>> Read More

PYRIMIDINE COMPOUNDS AS JAK KINASE INHIBITORS
(Fri, 03 Nov 2017)
The invention provides compounds of formula (I): wherein the variables are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are inhibitors of JAK kinases. The
invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat gastrointestinal and other inflammatory diseases, and processes and
intermediates useful for preparing such compounds.
>> Read More

ANALOGS OF YOHIMBINE AND USES THEREOF
(Fri, 03 Nov 2017)
The present disclosure provides compounds of Formulae (I-A), (ΙI'), (III-A), (IV'), and (V-A), wherein the compounds are derived from or based on yohimbine. The provided compounds may be useful in
treating or preventing a disease (e.g., proliferative disease, cancers, inflammatory diseases, autoimmune diseases, and infectious diseases) in a subject in need thereof. The present disclosure
provides methods of preparing compounds of Formulae (I-A), (ΙI'), (III-A), (IV'), and (V-A). Also provided are pharmaceutical compositions, kits, methods, and uses that include or involve a compound
described herein.
>> Read More

A NOVEL CHOLESTEROL METABOLITE, 5-CHOLESTEN-3,25-DIOL, DISULFATE (25HCDS) FOR THERAPY OF METABOLIC DISORDERS, HYPERLIPIDEMIA, DIABETES, FATTY LIVER DISEASES AND ATHEROSCLEROSIS
(Thu, 02 Nov 2017)
5-cholesten-3, 25-diol, disulfate (25HCDS) has been found to be an authentic PPAR ³ agonist and LXR antagonist, and is used for the therapy of lipid disorders and inflammatory diseases, including
without limitation fatty liver, inflammatory bowel, and atherosclerotic diseases.
>> Read More

HETEROBIFUNCTIONAL INHIBITORS OF E-SELECTINS AND CXCR4 CHEMOKINE RECEPTORS
(Fri, 27 Oct 2017)
<p id="p-0001" num="0000">Compounds, compositions, and methods for treatment and/or prevention of cancer and inflammatory diseases, and for releasing cells such as stem cells (e.g., bone marrow
progenitor cells) into circulating blood and enhancing retention of the cells in the blood are disclosed. For example, heterobifunctional compounds that inhibit both E-selectins and CXCR4 chemokine
receptors are described and pharmaceutical compositions comprising at least one of the same.</p>
>> Read More

BIOMARKERS AND METHODS FOR ASSESSING RESPONSE TO INFLAMMATORY DISEASE THERAPY
(Fri, 27 Oct 2017)
Provided herein are methods for assessing response to inflammatory disease therapy. The methods include performing immunoassays to generate scores based on quantitative data for expression of
biomarkers relating to inflammatory biomarkers to assess disease activity in inflammatory diseases, e.g., rheumatoid arthritis. Also provided are uses of inflammatory biomarkers for guiding treatment
decisions.
>> Read More

CONJUGATES COMPRISING RIPK2 INHIBITORS
(Fri, 27 Oct 2017)
The present invention relates to compounds, compositions, combinations and medicaments containing said compounds and processes for their preparation. The invention also relates to the use of said
compounds, combinations, compositions and medicaments, for example as inhibitors of the activity of RIP2 kinase, including degrading RIP2 kinase, the treatment of diseases and conditions mediated by
the RIP2 kinase, in particular for the treatment of inflammatory diseases or conditions.
>> Read More

4-(AZETIDIN-1-YL)PYRIMIDINE DERIVATIVES WITH ANTI-MITOTIC AND ANTI-PROLIFERATIVE ACTIVITY
(Fri, 20 Oct 2017)
The invention relates to 4-(azetidin-1-yl)pyrimidyl compounds of formula (I), wherein X and Y are, independently of each other CH or N; U is O, CHOH, CHCH2OH, C(CH3)OH, CO, CHNH2; R1 and R2 are,
independently of each other H, F or CH3; and R3 is H or CH3; and related compounds with anti-mitotic and anti-proliferative properties, and methods of making use of such compounds in therapy or
diagnostics to attenuate undesired cell proliferation, growth, migration, metastasis tumor formation, and inflammatory conditions. Additionally, methods are disclosed of treating diseases associated
with undesired angiogenesis and undesired proliferation, and methods of treating infectious and inflammatory diseases using such compounds.
>> Read More

BROMODOMAIN INHIBITORS
(Fri, 20 Oct 2017)
The present invention provides for compounds of formula (I) wherein R1, R2, R3, R4, R6, X1, and X2 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof,
that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, cancer, and AIDS. Also provided are pharmaceutical compositions comprising compounds of formula
(I).
>> Read More

PHENYL UREA DERIVATIVES AS N-FORMYL PEPTIDE RECEPTOR MODULATORS
(Fri, 20 Oct 2017)
The present invention relates to phenyl urea derivatives useful for the treatment of inflammatory diseases, pharmaceutical compositions containing them and their use as tools or as pharmaceuticals as
modulators of the N-formyl peptide receptor (FPR), including FPR1 and FPR2, or as selective agonists of the FPR1 receptor.
>> Read More

4-(AZETIDIN-1-YL)PYRIMIDINE DERIVATIVES WITH ANTI-MITOTIC AND ANTI-PROLIFERATIVE ACTIVITY
(Thu, 19 Oct 2017)
The invention relates to 4-(azetidin-1-yl)pyrimidyl compounds of formula (I), wherein X and Y are, independently of each other CH or N; U is O, CHOH, CHCH 2 OH, C(CH 3 )OH, CO, CHNH 2 ; R 1 and R 2
are, independently of each other H, F or CH 3 ; and R 3 is H or CH 3 ; and related compounds with anti-mitotic and anti-proliferative properties, and methods of making use of such compounds in
therapy or diagnostics to attenuate undesired cell proliferation, growth, migration, metastasis tumor formation, and inflammatory conditions. Additionally, methods are disclosed of treating diseases
associated with undesired angiogenesis and undesired proliferation, and methods of treating infectious and inflammatory diseases using such compounds.
>> Read More

KINASE INHIBITORS
(Fri, 13 Oct 2017)
<p id="p-0001" num="0000">There are provided compounds of formula I,</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001"
he="25.40mm" wi="75.61mm" file="US20170291917A1-20171012-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003"
num="0000">wherein T, A, Q, Z, G, R<sup>4</sup>, R<sup>5a</sup>, R<sup>5b </sup>and n have meanings given in the description, which compounds have
antiinflammatory activity (e.g. through inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase enzymes; Syk kinase; and members of the Src family of tyrosine
kinases) and have use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and
intestines.</p>
>> Read More

IL-17A/F HETEROLOGOUS POLYPEPTIDES AND THERAPEUTIC USES THEREOF
(Fri, 13 Oct 2017)
<p id="p-0001" num="0000">The present invention is directed to a novel naturally occurring human cytokine that is comprised of a heterodimer of interleukin-17 and interleukin-17F designated
herein as interleukin 17A/F (IL-17A/F). Also provided herein are vectors and host cells comprising those nucleic acid sequences, chimeric polypeptide molecules comprising the polypeptides of the
present invention fused to heterologous polypeptide sequences, specific antibodies which bind to the polypeptides of the present invention and to methods for producing the polypeptides of the present
invention. Further provided herein are methods for treating degenerative cartilaginous disorders and other inflammatory diseases.</p>
>> Read More

SMALL MOLECULE REGULATORS OF STEROID RECEPTOR COACTIVATORS AND METHODS OF USE THEREOF
(Fri, 13 Oct 2017)
Small molecule regulators of steroid receptor coactivator (SRC) family proteins are provided, as well as methods for their use in treating or preventing SRC-related diseases. The SRC-related diseases
can include cancer, metabolic disorders, human immunodeficiency virus, neurodegenerative disorders, and/or inflammatory diseases. Also provided are methods for regulating SRC family proteins in a
cell.
>> Read More

KINASE INHIBITORS
(Fri, 13 Oct 2017)
There are provided compounds of formula I, (I) wherein T, A, Q, Z, G, R4, R5a, R5b and n have meanings given in the description, which compounds have antiinflammatory activity (e.g. through
inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase enzymes; Syk kinase; and members of the Src family of tyrosine kinases) and have use in therapy, including
in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines.
>> Read More

PHARMACEUTICAL COMPOSITIONS AND THEIR USE FOR TREATMENT OF CANCER AND AUTOIMMUNE DISEASES
(Fri, 06 Oct 2017)
<p id="p-0001" num="0000">Described herein are combination therapies for cancer (such as lymphoid malignancies) and immune diseases (such as autoimmune diseases and inflammatory diseases). The
therapies comprise the combined use of inhibitors of BTK, mTOR kinase, and Bcl-2 or their signaling pathways, and immunomodulatory drugs. Also described are pharmaceutical compositions and kits
comprising these inhibitors.</p>
>> Read More

Bruton's Tyrosine Kinase Inhibitors
(Fri, 06 Oct 2017)
<p id="p-0001" num="0000">Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (BTK). Methods for the preparation of the compounds are disclosed. Also disclosed
are pharmaceutical compositions that include the compounds. Methods of using the BTK inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune
diseeases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.</p> <p id="p-0002" num="0000"><chemistry
id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="33.78mm" wi="53.68mm" file="US20170283393A1-20171005-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/>
</chemistry> </p>
>> Read More

PHENYL UREA DERIVATIVES AS N-FORMYL PEPTIDE RECEPTOR MODULATORS
(Fri, 06 Oct 2017)
The present disclosure relates to phenyl urea derivatives useful for the treatment of inflammatory diseases, pharmaceutical compositions containing them and their use as modulators of the N-formyl
peptide receptor (FPR), including FPRl and FPR2, or as selective agonists of the FPRl receptor.
>> Read More

BICYCLIC COMPOUND
(Thu, 05 Oct 2017)
Provided is a bicyclic compound having an acetyl-CoA carboxylase inhibitory action. A compound represented by the formula: wherein each symbol is as described in the DESCRIPTION, or a salt thereof
has an acetyl-CoA carboxylase inhibitory action, is useful for the prophylaxis or treatment of cancer, inflammatory diseases and the like, and has superior efficacy.
>> Read More

MODULATORS OF THE RETINOID-RELATED ORPHAN RECEPTOR GAMMA (ROR-GAMMA) FOR USE IN THE TREATMENT OF AUTOIMMUNE AND INFLAMMATORY DISEASES
(Thu, 21 Sep 2017)
The present invention relates to retinoid-related orphan receptor gamma (ROR³) modulators of formula (I)v for use in the treatment of autoimmune or inflammatory diseases.
>> Read More

NO- AND H2S- RELEASING COMPOUNDS
(Fri, 15 Sep 2017)
<p id="p-0001" num="0000">This disclosure relates to compounds containing both an NO-releasing moiety and an H<sub>2</sub>S-releasing moiety and the use of such compounds in
treating inflammatory diseases, including cancers.</p>
>> Read More

Bromodomain inhibitors
(Fri, 15 Sep 2017)
2 3 4 1 2 The present invention provides for compounds of formula (I) wherein A1 , A , A , A , X , X , Y L', G1 , R', and R1 have any of the values defined thereof in the specification, and
pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, cancer, and AIDS. Also provided are pharmaceutical
compositions comprising one or more compounds of formula (I).
>> Read More

BIOMARKERS AND METHODS FOR PREDICTING RESPONSE TO DISCONTINUATION OF INFLAMMATORY DISEASE THERAPY
(Sat, 09 Sep 2017)
Provided herein are methods for assessing response to inflammatory disease therapy. The methods include performing immunoassays to generate scores based on quantitative data for expression of
biomarkers relating to inflammatory biomarkers to predict flare and sustained remission. The methods further include recommending discontinuation of a therapeutic regimen, or no change in a
therapeutic regimen, based on the predictions generated by the quantitative data.
>> Read More

Bicyclic heteroaryl derivatives as MNK1 and MNK2 modulators and uses thereof
(Fri, 08 Sep 2017)
The present invention relates to certain compounds (e.g., imidazopyrazine, imidazopyridine, imidazopyridazine and imidazpyrimidine compounds) that act as inhibitors of the MAP kinase interacting
kinases MNK2a, MNK2b, MNKl a, and MNK1b. The present invention further relates to pharmaceutical compositions comprising these compounds, and to the use of the compounds for the preparation of a
medicament for the prophylaxis and treatment of diseases (e.g., proliferative diseases (e.g., cancer), inflammatory diseases, Alzheimer's disease), as well as methods of treating these diseases.
>> Read More

METHODS OF DETECTING AND TREATING AIRWAY INFLAMMATORY DISEASES
(Fri, 01 Sep 2017)
The present invention is related to novel methods for identifying and/or diagnosing and/or treating a population of subjects that are at risk for developing and/or have an inflammatory disease of the
airways, including type 2 cytokine-driven airway inflammation.
>> Read More

CONJUGATES OF PORPHYRINOID PHOTOSENSITIZERS AND GLYCEROL-BASED POLYMERS FOR PHOTODYNAMIC THERAPY
(Thu, 31 Aug 2017)
Biologically active compounds that can be used as photosensitizers for diagnostic and therapeutic applications, particularly for PDT of cancer, infections and other hyperproliferative diseases,
fluorescence diagnosis and PDT treatment of a non-tumorous indication such as arthritis, inflammatory diseases, viral or bacterial infections, dermatological, ophthalmological or urological disorders
are provided as well as providing methods to obtain them in pharmaceutical quality. In addition, conjugates are provided in which these photosensitizers are attached to water-soluble polymers via
cleavable linkers that can be cleaved in the body under specific conditions. Another embodiment consists of formulating the desired tetrapyrrole photosensitizer into a pharmaceutical formulation to
be injected into the body avoiding undesirable effects like solubility problems or delayed pharmacokinetics of the tetrapyrrole systems.
>> Read More

6-HETEROCYCLYL-4-MORPHOLIN-4-YLPYRIDINE-2-ONE COMPOUNDS USEFUL FOR THE TREATMENT OF CANCER AND DIABETES
(Fri, 25 Aug 2017)
The invention provides novel 6-heterocyclyl-4-morpholin-4-yl-pyridine-2-one compounds of formula (I), pharmaceutical compositions containing such compounds, and methods for using such compounds in
treatment of diseases including cancer, diabetes, inflammatory disease, neurodegenerative disorders, cardiovascular disorders and viral infections; wherein R1, R2, R3 and A are as defined in the
specification.
>> Read More

6-ARYL-4-MORPHOLIN-1-YLPYRIDONE COMPOUNDS USEFUL FOR THE TREATMENT OF CANCER AND DIABETES
(Fri, 25 Aug 2017)
The invention provides novel 6-aryl or 6-heteroaryl 4-morpholin-4-yl-pyhdine-2-one compounds of formula (I), pharmaceutical compositions containing such compounds, and methods for using such
compounds in treatment of diseases including cancer, diabetes, inflammatory diseases, neurodegenerative disorders, cardiovascular disorders and viral infections; wherein R1, R2, R3 and R4 are as
defined in the specification.
>> Read More

METHODS AND COMPOSITIONS FOR T CELL GENERATION AND USES THEREOF
(Fri, 18 Aug 2017)
<p id="p-0001" num="0000">Among the various aspects of the present disclosure is the provision of a method of treating an inflammatory bowel disease. Another aspect provides the provision of a
screening method for therapeutic agents. Another aspect provides a method of detecting T<sub>reg </sub>cells to determine if a subject has an inflammatory disease. The present disclosure
provides for methods of treatment, diagnosis, and screening for drugs for colitis and ileitis.</p>
>> Read More

Kinase inhibitors
(Wed, 16 Aug 2017)
<p id="p-0001" num="0000">In compounds of formula I:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="51.31mm" wi="75.18mm"
file="US09732063-20170815-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> R<sup>1 </sup>to R<sup>5</sup>, Ar and
X<sup>1 </sup>to X<sup>3 </sup>have defined meanings. The compounds have anti-inflammatory activity (e.g., through inhibition of one or more of members of: the family of p38
mitogen-activated protein kinase enzymes; Syk kinase; and members of the Src family of tyrosine kinases) and have use in therapy, including in pharmaceutical combinations, especially in the treatment
of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines. </p>
>> Read More

Beta 2-AR exciting and anti-inflammatory dual-function alkaloid and application thereof
(Wed, 16 Aug 2017)
The invention discloses alkaloid as shown in the formula I or II and an analogue, an isomer, a despinner or a derivative thereof, and the the formula I or II is shown in the specification. The
compound is separated from purslane, and a research shows that the compound has beta 2-AR exciting and anti-inflammatory dual-function activity; an available compound is provided for treatment of
respiratory system diseases such as asthma and relevant inflammatory diseases.
>> Read More

NRF2 ACTIVATING COMPOUNDS AND USES THEREOF
(Fri, 11 Aug 2017)
Aspects of the present disclosure include compounds that activate Nrf2. Such compounds find use in the treatment of autoimmune and inflammatory diseases and disorders, such as for example psoriasis
and multiple sclerosis. Embodiments of the present disclosure also relate to pharmaceutical compositions that include these compounds, methods of using these compounds in the treatment of various
diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
>> Read More

NRF2 ACTIVATING COMPOUNDS AND USES THEREOF
(Fri, 11 Aug 2017)
Aspects of the present disclosure include compounds that activate Nrf2. Such compounds may find use in the treatment of autoimmune and inflammatory diseases and disorders, such as for example
psoriasis and multiple sclerosis. Embodiments of the present disclosure also relate to pharmaceutical compositions that include these compounds, methods of using these compounds in the treatment of
various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
>> Read More

CCR9 ANTAGONIST COMPOUNDS
(Fri, 04 Aug 2017)
<p id="p-0001" num="0000">Provided herein are compounds that inhibit CCR9 receptor function. Also provided herein are methods of treating inflammatory disease in a subject, comprising
administering to the subject a compound of the invention. Accordingly, in one aspect, provided herein is a compound of Formula (1) or a pharmaceutically acceptable salt thereof. In another aspect,
provided herein is a pharmaceutical composition, comprising a compound of Formula (1), and a pharmaceutically acceptable carrier.</p>
>> Read More

Nrf2 activating compounds and uses thereof
(Fri, 04 Aug 2017)
<p id="p-0001" num="0000">Aspects of the present disclosure include compounds that activate Nrf2. Such compounds find use in the treatment of autoimmune and inflammatory diseases and disorders,
such as for example psoriasis and multiple sclerosis. Embodiments of the present disclosure also relate to pharmaceutical compositions that include these compounds, methods of using these compounds
in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.</p>
>> Read More

Nrf2 activating compounds and uses thereof
(Fri, 04 Aug 2017)
<p id="p-0001" num="0000">Aspects of the present disclosure include compounds that activate Nrf2. Such compounds may find use in the treatment of autoimmune and inflammatory diseases and
disorders, such as for example psoriasis and multiple sclerosis. Embodiments of the present disclosure also relate to pharmaceutical compositions that include these compounds, methods of using these
compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.</p>
>> Read More

A kind of a substituted quinazoline-4-ketone compound and a preparation method and medical application thereof
(Wed, 02 Aug 2017)
The invention relates to a new PI3K[delta] inhibitor compound shown as the general formula I and having a substituted quinazoline-4-ketone structure, a preparation method of the compound, and an
application of the compound to prepare a medicine for preventing and/or treating PI3K[delta]-related diseases, which include tumor and inflammatory diseases.
>> Read More

Bromine structural-domain inhibitor
(Sat, 29 Jul 2017)
The invention relates to a bromine structural-domain inhibitor, provides a compound shown as a formula (I) and pharmaceutically acceptable salt of the compound and further provides a medicine
composition with the compound shown in the formula (I) or a plurality of compounds shown in the formula (I). An A<1>, an A<2>, an A<3>, an A<4>, an X<1>, an X<2>,
a Y<1>, an L<1>, a G<1>, an R<x> and an R<y> have values defined in optional instruction books. The compound can be used as a preparation for treating diseases and
disease states including inflammatory diseases, cancer and AIDS (acquired immune deficiency syndrome).
>> Read More

KINASE INHIBITORS
(Fri, 28 Jul 2017)
<p id="p-0001" num="0000">Compounds of formula I,</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="34.12mm" wi="74.93mm"
file="US20170209445A1-20170727-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">have anti-inflammatory activity.
Exemplary mechanisms of action include inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase enzymes; Syk kinase; and members of the Src family of tyrosine
kinases. The compounds have use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and
intestines.</p>
>> Read More

METHODS AND SYSTEMS FOR PROCESSING PARTICLES
(Fri, 28 Jul 2017)
<p id="p-0001" num="0000">Described herein are improved microfluidic devices and methods for processing cells that can improve cell quality, streamline workflows, and lower costs. Applications
include research and clinical diagnostics in cancer, infectious disease, and inflammatory disease, among other disease areas.</p>
>> Read More

IRAK4 INHIBITING AGENTS
(Fri, 28 Jul 2017)
Provided are compounds of Formula I, or pharmaceutically acceptable salts thereof, and methods for their use and production. Formula (I) The compounds are IRAK-4 inhibitors useful for treating an
inflammatory disease, an autoimmune disease, cancer, a cardiovascular disease, a disease of the central nervous system, a disease of the skin, an ophthalmic disease and condition, and a bone disease.
>> Read More

QUINOLINE DERIVATIVES FOR THE TREATMENT OF INFLAMMATORY DISEASES
(Fri, 21 Jul 2017)
<p id="p-0001" num="0000">The present invention relates to a compound of formula (I) wherein: Formula (II) means an aromatic ring wherein V is C or N and when V is N; Q is N or O, provided that
R″ does not exist when Q is O; R′ independently represent a hydrogen atom or a group chosen among a (C<sub>1</sub>-C<sub>3</sub>)alkyl group, a halogen atom, a hydroxy! group,
a —COOR<sub>1 </sub>group, a —NO2 group, a —NR<sub>1</sub>R<sub>2 </sub>group, a morpholinyl or a morpholino group, a N-methylpiperazinyl group, a
(C<sub>1</sub>-C3)fluoroalkyl group, a —O—P(=O)—(OR<sub>3</sub>XOR<sub>4</sub>) group, a (C<sub>1</sub>-C<sub>4</sub>)alkoxy group and a
—CN group, and can further be a group chosen among: (IIa), (IIIa) or anyone of its pharmaceutically acceptable salt, for use in the treatment and/or prevention of an inflammatory disease.</p>
<p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="98.13mm" wi="65.28mm" file="US20170204063A1-20170720-C00001.TIF" alt="embedded image"
img-content="chem" img-format="tif"/> </chemistry> </p>
>> Read More

INHIBITORS OF HISTONE DEACETYLASE
(Fri, 21 Jul 2017)
<p id="p-0001" num="0000">This invention provides compounds that are inhibitors of HDAC2. The compounds (e.g., compounds according to Formula (I), (II), (IIa), (III), (IV), (V), or (VI))
accordingly are useful for treating, alleviating, or preventing a condition in a subject such as a neurological disorder, memory or cognitive function disorder or impairment, extinction learning
disorder, fungal disease or infection, inflammatory disease, hematological disease, or neoplastic disease, or for improving memory or treating, alleviating, or preventing memory loss or
impairment.</p>
>> Read More

QUINAZOLIN-4 (3H)-ONE DERIVATIVES USED AS P13 KINASE INHIBITORS
(Fri, 21 Jul 2017)
<p id="p-0001" num="0000">The present invention relates to the compound of formula (I)</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img
id="EMI-C00001" he="68.41mm" wi="61.04mm" file="US20170202841A1-20170720-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003"
num="0000">and to compositions comprising the same and to the use of the compound and to compositions of the compound in treatment, for example in the treatment of inflammatory diseases, in
particular respiratory inflammatory disease. The invention also extends to methods of making the said compound.</p>
>> Read More

Compounds for the treatment of cancer and inflammatory diseases
(Fri, 21 Jul 2017)
<p id="p-0001" num="0000">The present invention relates to novel compounds and pharmaceutical compositions thereof which may be useful in the treatment and/or prevention of various conditions.
The present invention also provides methods of preparing such compounds and compositions, and methods of using the same.</p>
>> Read More

CRYSTAL FORMS OF IMMUNOMODULATORY DRUG POMALIDOMIDE AND CO-CRYSTAL WITH GENTISIC ACID
(Fri, 21 Jul 2017)
The present invention relates to novel solid crystal forms of Pomalidomide named Form B, Form M, Pomalidomide: Gentisic acid co-crystal and their preparation. Advantageously, these solid forms are
used in pharmaceutical compositions for the treatment and the prevention of multiple myeloma, of inflammatory diseases, of autoimmune diseases, of immune diseases, of myelodysplastic syndrome, of
myeloproliferative disorders, of anemia, of scleroderma, amyloidosis or of other diseases associated with unwanted angiogenesis.
>> Read More

A QUINOLINE DERIVATIVE FOR THE TREATMENT OF INFLAMMATORY DISEASES AND AIDS
(Fri, 14 Jul 2017)
<p id="p-0001" num="0000">The present invention relates to a compound of formula (1) in the form of a base or addition salt with an acid, particularly a pharmaceutically acceptable acid. It
further relates to a pharmaceutical composition including the compound and at least one pharmaceutically acceptable excipient, to a process for preparing said compound and to a corresponding
intermediate compound.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="32.77mm" wi="73.32mm"
file="US20170197938A1-20170713-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
>> Read More

Heterocyclic GSK-3 allosteric modulators
(Fri, 14 Jul 2017)
<p id="p-0001" num="0000">The present invention relates to heterocyclic substituted quinoline derivatives as allosteric inhibitors of the glycogen synthase kinase-3 (GSK-3) enzyme. Therefore,
these compounds are useful for the manufacturing of a medicament designed for the treatment and/or prevention of diseases wherein GSK-3 is involved, such as neurodegenerative diseases, inflammatory
diseases, cancer, diabetes, and to promote various regenerative processes.</p>
>> Read More

ANTIBODIES THAT BIND AND BLOCK TRIGGERING RECEPTOR EXPRESSED ON MYELOID CELLS-1 (TREM-1)
(Fri, 07 Jul 2017)
<p id="p-0001" num="0000">The invention relates to antibodies that are capable of specifically binding TREM-1 and preventing the activation of TREM-1, a protein expressed on monocytes,
macrophages and neutrophils. Such antibodies find utility in the treatment of individuals with an inflammatory disease, such as rheumatoid arthritis and inflammatory bowel disease.</p>
>> Read More

MULTICYCLIC COMPOUNDS AND USES THEREOF
(Fri, 07 Jul 2017)
The present invention relates to multicyclic compounds containing a urea or a guanidine moiety, or pharmaceutically acceptable salts or compositions thereof represented by Structural Formula (IA) or
a pharmaceutically acceptable salt thereof and pharmaceutical comopositions comprising the multicyclic compounds. The invention also relates to a method for treating a disease or disorder selected
from cancer (e.g., lymphoma, such as mantle cell lymphoma), a neurodegenerative disease, an inflammatory diseases or an immune system disease (e.g., a T-Cell mediated autoimmune disesase) in a
subject in need thereof. The method comprises administering to a subject in need thereof a therapeutically effective amount of a compound of the invention, or a pharmaceutically acceptable salt
thereof, or a composition comprising a compound of the invention, or a pharmaceutically acceptable salt thereof.
>> Read More

COMBINATION THERAPIES FOR HEMATOLOGIC MALIGNANCIES
(Thu, 06 Jul 2017)
The invention provides methods that relate to a novel therapeutic strategy for the treatment of hematological malignancies and inflammatory diseases. In particular, the method comprises
administration of a compound of formula A, wherein R is H, halo, or C1-C6 alkyl; R' is C1-C6 alkyl; or a pharmaceutically acceptable salt thereof; and optionally a pharmaceutically acceptable
excipient; and one or more additional therapeutic agents optionally selected from the group consisting of bendamustine, rituximab, and ofatumumab.
>> Read More

HETEROCYCLIC COMPOUND
(Thu, 06 Jul 2017)
The present invention provides a heterocyclic compound having a HDAC inhibitory action, and useful for the treatment of autoimmune diseases and/or inflammatory diseases, graft versus host disease,
cancers, central nervous diseases including neurodegenerative diseases and the like, and a medicament comprising the compound. The present invention relates to a compound represented by the formula
(I): wherein each symbol is as defined in the specification, or a salt thereof.
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Prenylated flavonoid, and applications thereof in preparing drugs used for treating inflammatory diseases
(Wed, 05 Jul 2017)
The invention relates to a prenylated flavonoid, and applications thereof in preparing drugs used for treating inflammatory diseases. The prenylated flavonoid is a novel compound separated from
artocarpus heterophyllus of Artocarpus, Moraceae, and is named as artoheteroid C. The structure of artoheteroid C is disclosed in the invention, possesses high inhibition activity on mouse neutrophil
respiratory burst, can be used for preparing drugs used for treating inflammatory diseases, and can be used for clinical treatment of oxidative damages, such as rheumatoid arthritis, compensatory
anti-inflammatory response syndrome, and systemic inflammatory response syndrome, caused by neutrophil excessive activation; and the IC50 value is 7.5<mu>M.
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COMPOSICIONES DE CICLODEXTRINA Y DERIVADOS DE BUDESONIDA Y METODOS.
(Wed, 05 Jul 2017)
The present invention relates to novel and useful pharmaceutical compositions formulated with a cyclodextrin compound and a budesonide derivative for the treatment and/or prevention of pulmonary
inflammatory disease. The present invention also relates to a novel and useful analytical technique for the detection and the quantification of HP-ß-CD in solution. More specifically, the present
invention relates to the use of a validated 1H NMR analysis for the detection and quantification of cyclodextrins directly in pharmaceutical formulations without any extraction or separation steps
for liquid formulations.
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NOVEL SESQUITERPENE DERIVATIVES AND THEIR USE IN INFLAMMATION OR CANCER TREATMENT
(Fri, 30 Jun 2017)
<p id="p-0001" num="0000">A new class of sesquiterpene derivative useful for treating cancerous and inflammatory diseases are disclosed. These deoxyelephantopin derivatives are effective in
suppressing proliferation, migration, mobility, invasion, growth, and/or metastasis of cancer cells in a patient, or useful for enhancing an anti-proliferative effect of another anti-cancer drug on
cancer cells when treating a patient, or for sensitizing and/or enhancing an anti-cancer effect of a gluthathione synthesis blocker on inhibition of triple negative breast cancer cell activity, or
for treatment and/or prophylaxis of lipopolysaccharide-stimulated inflammatory response in a patient, or for all of the above. Also disclosed are methods of preparing the deoxyelephantopin
derivatives.</p>
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METHOD FOR PRODUCING MONOMETHYL FUMARATE COMPOUNDS
(Fri, 30 Jun 2017)
The present invention relates to a novel method for preparing monomethyl fumarate, which can preferably be used in the treatment and/or prevention of systemic diseases, autoimmune diseases,
inflammatory diseases such as multiple sclerosis and psoriasis. Further, the present invention relates to the use of specific compounds as intermediates in the process for preparing a monomethyl
fumarate prodrug.
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COMPOUNDS FOR THE TREATMENT OF CANCER AND INFLAMMATORY DISEASE
(Fri, 30 Jun 2017)
Provided herein are compounds that inhibit the phosphorylation of MAPK and thus are compositions and methods for treating cancer and inflammatory disease.
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IMMUNE CELL-TARGETED PARTICLES
(Fri, 30 Jun 2017)
The present disclosure provides particles with a polymeric core containing a pharmaceutically active agent; and an antibody fragment conjugated to the surface of the particle, wherein the antibody
fragment targets an endogenous immune cell subset (e.g., an endogenous T-cell or a myeloid-derived suppressor cell). The present invention provides methods for forming and methods for using the
particles. The particles described herein may be useful in treating and/or preventing proliferative disease, inflammatory disease, or neoplastic disorders (e.g., cancer, autoimmune diseases). Also
provided in the present disclosure are pharmaceutical compositions, kits, methods, and uses including or using a particle described herein.
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GLYCOSYLATED INDOLOCARBAZOLES, METHOD FOR OBTAINING SAME AND USES THEREOF
(Thu, 29 Jun 2017)
Glycosylated indolocarbazoles of formula (II), method for obtaining same and uses thereof. This invention relates to rebeccamycin and staurosporine derivatives obtained by fermentation of recombinant
bacterial strains. The invention also relates to the methods used to obtain the recombinant strains and the production of rebeccamycin and staurosporine derivatives. The invention also relates to
bacterial strains that are of use for the production of rebeccamycin and staurosporine derivatives. Lastly, the rebeccamycin and staurosporine derivatives described herein are applicable to the field
of human health, specifically for manufacturing drugs that are of use in the treatment of tumour, neurological and inflammatory diseases.
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2-phenylbenzofuran derivatives, method for preparing the same and use of the same for treating inflammatory disease
(Fri, 23 Jun 2017)
<p id="p-0001" num="0000">The present invention relates to a novel 2-phenylbenzofuran derivative or a pharmaceutically acceptable salt thereof, a production method for the same, and a
pharmaceutical composition for preventing or treating an inflammatory disease comprising the same as an active ingredient, and the novel 2-phenylbenzofuran derivative or the pharmaceutically
acceptable salt thereof according to the present invention is outstandingly effective in suppressing NO, IL-6, and TNF-alpha induced by macrophages, and therefore can advantageously be used in a
pharmaceutical composition for preventing or treating an inflammatory disease.</p>
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COMPOUNDS FOR THE TREATMENT OF CANCER AND INFLAMMATORY DISEASE
(Fri, 23 Jun 2017)
<p id="p-0001" num="0000">Provided herein are compounds that inhibit the phosphorylation of MAPK and thus are useful in compositions and methods for treating cancer and inflammatory
disease.</p>
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HETEROARYL AMIDE SULTAM DERIVATIVES AS RORc MODULATORS
(Fri, 23 Jun 2017)
Compounds of the formula I: (I) or a pharmaceutical salt thereof, wherein m, n, p, q, Het, A, W, R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 are as defined herein. Also disclosed are methods of making
the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.
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SMALL MOLECULES AGAINST CANCER
(Fri, 23 Jun 2017)
Compounds capable of, or usable in, killing cancer cells, and/or modulating a biological activity of a chemokine, and/or inhibiting a kinase, and/or treating diseases and disorders associated with a
biological activity of a chemokine and/or cell migration, and/or treating disease and disorders such as cancer and inflammatory diseases and disorders, are provided herein. The compounds are listed
in Tables 2, 4 and 5, and/or are represented by Formulae I, IV, V and VI, as defined in the specification. Methods utilizing these compounds are also provided.
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SMALL MOLECULES FOR INHIBITING CHEMOKINE ACTIVITY, A KINASE ACTIVITY AND/OR CANCER CELLS GROWTH
(Fri, 23 Jun 2017)
Compounds capable of, or usable in, inducing death of cancer cells and/or modulating a biological activity of a chemokine e.g., cell migration, and/or treating diseases and disorders associated with
a biological activity of a chemokine and/or cell migration, and/or inhibiting a kinase and/or in treating a disease or disorder associated with an activity of a kinase, such as cancer and
inflammatory diseases and disorders, are provided herein. The compounds are collectively represented by Formulae (Ia) or (Ib): wherein A, B D, E, G and R1-R5 are as defined in the specification.
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METHODS FOR IDENTIFYING INHIBITORS OF "STIMULATOR OF INTERFERON GENE"-DEPENDENT INTERFERON PRODUCTION
(Fri, 23 Jun 2017)
The present invention relates to the use cyclic-di-nucleotide and related scaffold molecules that measurably inhibit STING signaling, and methods for their use in identifying more potent inhibitors
of STING signaling. In particular, the methods provided can be used to identify potent inhibitors of STING signaling, which are useful in the treatment of autoimmune and inflammatory diseases. Also
provided are compounds having STING inhibitory activity useful in the treatment of autoimmune and inflammatory diseases.
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IL-17A/F HETERODIMERIC POLYPEPTIDES AND THERAPEUTIC THEREOF
(Thu, 22 Jun 2017)
The present invention is directed to a novel naturally occurring human cytokine that is comprised of a heterodimer of interleukin-17 and interleukin-17F designated herein as interleukin 17A/F (IL-17
A/F). Also provided herein are vectors and host cells comprising those nucleic acid sequences, chimeric polypeptide molecules comprising the polypeptides of the present invention fused to
heterologous polypeptide sequences, specific antibodies which bind to the polypeptides of the present invention and to methods for producing the polypeptides of the present invention. Further
provided herein are methods for treating degenerative cartilaginous disorders and other inflammatory diseases.
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CARBAZOLE COMPOUNDS AND THERAPEUTIC USES OF THE COMPOUNDS
(Fri, 16 Jun 2017)
<p id="p-0001" num="0000">Compounds of the general structural formula (I) and (II) and use of the compounds and salts and hydrates thereof, as therapeutic agents are disclosed. Treatable
diseases and conditions include cancers, inflammatory diseases and conditions, and immunodeficiency diseases. (I), (II).</p>
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Biomarkers and Methods for Measuring and Monitoring Inflammatory Disease Activity
(Fri, 16 Jun 2017)
<p id="p-0001" num="0000">Biomarkers useful for diagnosing and assessing inflammatory disease are provided, along with kits for measuring their expression. The invention also provides
predictive models, based on the biomarkers, as well as computer systems, and software embodiments of the models for scoring and optionally classifying samples. The biomarkers include at least two
biomarkers selected from the DAIMRK group and the score is a disease activity index (DAI).</p>
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3-heteroaroylamino-propionic acid derivatives and their use as pharmaceuticals
(Fri, 16 Jun 2017)
3-Heteroaroylamino-propionic acid derivatives and their use as pharmaceuticals The present invention relates to compounds of the formula I, wherein Ht, G, R10, R30 , R40 , R50 and R60 have the
meanings indicated in the claims, which are valuable pharmaceutical active compounds. They are inhibitors of the protease cathepsin A, and are useful for the treatment of diseases such as
atherosclerosis, heart failure, renal diseases, liver diseases or inflammatory diseases, for example. The invention furthermore relates to processes for the preparation of the compounds of the
formula I, their use and pharmaceutical compositions comprising them.
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GADD45BETA TARGETING AGENTS
(Thu, 15 Jun 2017)
Compounds based around tetrapeptide, tripeptide and dipeptide moeties and corresponding peptiod moeties. Related methods and pharmaceutical compositions for use in treatment of cancer, inflammatory
diseases, and other disorders.
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3-(5-SUBSTITUTED-4-OXOQUINAZOLIN-3(4H)-YL)-3-DEUTERO-PIPERIDINE-2,6-DIONE DERIVATIVES AND COMPOSITIONS COMPRISING AND METHODS OF USING THE SAME
(Fri, 09 Jun 2017)
<p id="p-0001" num="0000">The invention provides 3-deuterium-enriched 3-(5-substituted-4-oxoquinazolin-3(4H)-yl)-piperidine-2,6-diones, deuterated derivatives thereof, stereoisomers thereof,
pharmaceutically acceptable salt forms thereof, and methods of treatment using the same, such as in the treatment of cancer, an immune-related disease, or an inflammatory disease.</p>
>> Read More

BINDING INHIBITOR BETWEEN TCTP DIMER TYPE IGE-DEPENDENT HISTAMINE RELEASING FACTOR AND RECEPTOR THEREOF, AND USE THEREOF
(Fri, 09 Jun 2017)
<p id="p-0001" num="0000">The present invention relates to a receptor-binding domain of an IgE-dependent histamine releasing factor (HRF), and a use thereof, and more specifically, ascertains,
as an HRF structual region, and a FL domain and an H2 domain which bind to a receptor of HRF existing in a cell membrane, ascertains the C-terminus domain of the HRF, and ascertains that a material
binding thereto inhibits IL-8 secretion, thereby determining that the FL and H2 domains and the C-terminus domain can be utilized in: the development of a therapeutic agent for treatment and
prevention of HRF-related disease including allergic diseases such as asthma, bronchitis, chronic obstructive pulmonary disease, bronchiectasis, rhinitis, atopic dermatitis, hives (urticaria), hay
fever, conjunctivitis, and anaphylaxis; inflammatory diseases such as bronchitis, pneumonia, arthritis, nephritis, psoriasis, dermatitis, Crohn's disease, enteritis, gingivitis, arteriosclerosis,
coronary arteritis, hepatitis, Behcet's disease, bladder cancer, prostatitis, pyelonephritis, glomerulonephritis, osteomyelitis, thyroiditis, uveitis, abdominal cavity inflammation, meningitis,
pulmonary fibrosis and rheumatoid arthritis; and malaria, and a method for screening for the HRF-related diseases.</p>
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PROCESSES FOR THE PREPARATION OF (R)-2-(7-(4-CYCLOPENTYL-3-(TRIFLUOROMETHYL)BENZYLOXY)-1,2,3,4-TETRAHYDROCYCLOPENTA[B]INDOL-3-YL)ACETIC ACID AND SALTS THEREOF
(Fri, 09 Jun 2017)
<p id="p-0001" num="0000">The present invention relates to processes and intermediates useful in the preparation of
(R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid of Formula (Ia) and salts thereof, an S1P1 receptor modulator that is useful in the
treatment of S1P1 receptor-associated disorders, for example, diseases and disorders mediated by lymphocytes, transplant rejection, autoimmune diseases and disorders, inflammatory diseases and
disorders (e.g., acute and chronic inflammatory conditions), cancer, and conditions characterized by an underlying defect in vascular integrity or that are associated with angiogenesis such as may be
pathologic (e.g., as may occur in inflammation, tumor development and atherosclerosis).</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img
id="EMI-C00001" he="36.49mm" wi="75.69mm" file="US20170159088A1-20170608-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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Alpha-7 nicotinic acetylcholine receptor modulators and uses thereof-I
(Fri, 09 Jun 2017)
<p id="p-0001" num="0000">The present invention relates to chemical compounds of formula (I), with the substituents as described in the specification, useful in the positive modulation of the
alpha 7 nicotinic acetylcholine receptor (α7 nAChR). The invention also relates to the use of these compounds in the treatment or prevention of a broad range of diseases in which the positive
modulation of α7 nAChR is advantageous, including neurodegenerative and neuropsychiatric diseases and also neuropathic pain and inflammatory diseases.</p> <p id="p-0002"
num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="19.90mm" wi="29.04mm" file="US09790173-20171017-C00001.TIF" alt="embedded image" img-content="chem"
img-format="tif"/> </chemistry> </p>
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HOMOBISPIPERIDINYL DERIVATIVES AS LIVER X RECEPTOR BETA AGONISTS, COMPOSITIONS, AND THEIR USE
(Fri, 09 Jun 2017)
In its many embodiments, the present invention provides certain substituted bispiperidinyl compounds of the Formula (I): and pharmaceutically acceptable salts thereof, wherein ring A, ring B, R1, R2,
R3, L, R4, X, Z, Li, Q and R5 are as defined herein. The novel compounds of the invention, and pharmaceutically acceptable compositions comprising a compound thereof, are useful as Liver Χ-β receptor
(LXRβ) agonists, and may be useful for treating or preventing pathologies related thereto. Such pathologies include, but are not limited to, inflammatory diseases and diseases characterized by
defects in cholesterol and lipid metabolism, such as Alzheimer's disease.
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ANTI-OX40 ANTIBODIES AND METHODS OF USE THEREOF
(Fri, 09 Jun 2017)
The present disclosure provides antibodies that specifically bind to human OX40 receptor (OX40) and compositions comprising such antibodies. In a specific aspect, the antibodies specifically bind to
human OX40 and modulate OX40 activity, e.g., enhance, activate, or induce OX40 activity, or diminish, deactivate, or suppress OX40 activity. The present disclosure also provides methods for treating
disorders, such as cancer, by administering an antibody that specifically binds to human OX40 and modulates OX40 activity, e.g., enhances, activates, or induces OX40 activity. Also provided are
methods for treating autoimmune or inflammatory diseases or disorders, by administering an antibody that specifically binds to human OX40 and modulates OX40 activity, e.g., diminishes, deactivates,
or suppresses OX40 activity.
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ANTI-GITR ANTIBODIES AND METHODS OF USE THEREOF
(Fri, 09 Jun 2017)
The present disclosure provides antibodies that specifically bind to human GITR, as well as compositions comprising such antibodies. In a specific aspect, the antibodies specifically bind to human
GITR and deactivate, reduce, or inhibit GITR activity. The present disclosure also provides methods for treating autoimmune or inflammatory diseases disorders, by administering an antibody that
specifically binds to human GITR and deactivates, reduces, or inhibits GITR activity.
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LIPID COMPOUNDS AND COMPOSITIONS AND THEIR OPTHALMIC USE
(Fri, 09 Jun 2017)
The invention relates to lipid compounds of formula (I) and their pharmaceutically acceptable salts for the prevention and/or treatment of ophthalmic disorders such as retinal degenerative disorders
and ocular inflammatory diseases: (I) (wherein R1 is either a C9 to C22 alkyl group, or a C9 to C22 alkenyl group having from 1 to 6 double bonds; R2 is selected from the group consisting of a
halogen atom, a hydroxy group, an alkyl group, an alkoxy group, an alkylthio group, a carboxy group, an acyl group, an amino group, and an alkylamino group; R3 is a hydrogen atom, or a group R2; R4
is a carboxylic acid or a derivative thereof; and X is methylene (-CH2-), or an oxygen or sulfur atom).
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PHARMACEUTICAL FORMULATIONS
(Fri, 02 Jun 2017)
Disclosed herein is glutathione in conjunction with an isoselenazol or isothiazol derivative, e.g., ebselen or ebsulfur derivative, to treat diabetes, lupus, or other chronic inflammatory disease.
The glutathione is preferably provided in a rapid release oral formulation that presents the glutathione for absorption in the first part of the ileum. The isoselenazol or isothiazol derivative is
preferably provided in a delayed release formulation to avoid overlapping high enteric concentration. These may be provided within the same unit dosage form.
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Methods of Treating Cancers, Immune and Autoimmune Diseases, and Inflammatory Diseases Based on BTK Occupancy and BTK Resynthesis Rate
(Fri, 26 May 2017)
<p id="p-0001" num="0000">In an embodiment, therapeutic methods and uses of Bruton's Tyrosine Kinase (BTK) inhibitors for treatment of cancer, inflammation, immune disorders, and autoimmune
disorders, including dermatoses, and for transplantation prophylaxis, based on BTK occupancies and/or BTK resynthesis rates for B cells in various diseases, tissue compartments, including bone marrow
and lymph nodes, are described. In an embodiment, dosing regimens for a BTK inhibitor for treatment of cancer, inflammation, immune disorders, and autoimmune disorders, including dermatoses, and for
transplantation prophylaxis, based on BTK occupancies and/or BTK resynthesis rates for B cells in various diseases, tissue compartments, including bone marrow and lymph nodes, are
described.</p>
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A novel compound (ks 513) isolated from pseudolysimachion rotundum var. subintegrum, the composition comprising the same as an active ingredient for preventing or treating allergy disease, inflammatory disease, asthma or chronic obstructive pulmonary disease and the use thereof
(Thu, 25 May 2017)
The present invention relates to a novel
(1aS,1bS,2S,4S,5aR,6S,6aS)-1a-(hydroxymethyl)-4-methoxy-2-(((2S,3R,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)oxy)octahydrooxireno[2',3':4,5]cyclopenta[1,2-c]pyran-6-yl
4-hydroxybenzoate} (KS-513), the isomer thereof, the pharmaceutically acceptable salt or solvates thereof, a composition comprising the same as an active ingredient for preventing or treating
allergic disease, inflammatory disease, asthma or chronic obstructive pulmonary disease (COPD) and the use thereof.
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SUBSTITUTED PYRAZOLOPYRIDINAMINES
(Fri, 19 May 2017)
The present invention relates to substituted pyrazolopyridinamine compounds of general formula (I) as described and defined herein, to methods of preparing said compounds, to intermediate compounds
useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the
treatment or prophylaxis of a disease, in particular of a hyperproliferative, angiogenesis disorders, inflammatory diseases or diseases associated with inflammatory pain, as a sole agent or in
combination with other active ingredients.
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CYANOPYRIDINE DERIVATIVES AS LIVER X RECEPTOR BETA AGONISTS, COMPOSITIONS, AND THEIR USE
(Fri, 19 May 2017)
In its many embodiments, the present invention provides substituted cyanopyridine containing compounds of the Formula (I): and acceptable salts thereof, wherein R1, R2, R3, R4, R5, X, Y, Q, and the
moiety are as defined herein. The novel compounds of the invention, and pharmaceutically acceptable compositions comprising a compound thereof, are useful as Liver X-β receptor (LXRβ) agonists, and
may be useful for treating or preventing pathologies related thereto. Such pathologies include, but are not limited to, inflammatory diseases and diseases characterized by defects in cholesterol and
lipid metabolism, such as Alzheimer's disease.
>> Read More

BISPIPERIDINYL DERIVATIVES AS LIVER X RECEPTOR BETA AGONISTS, COMPOSITIONS, AND THEIR USE
(Fri, 19 May 2017)
In its many embodiments, the present invention provides certain substituted bispiperidinyl compounds of the Formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, L, R4, Q
and R5 are as defined herein. The novel compounds of the invention, and pharmaceutically acceptable compositions comprising a compound thereof, are useful as Liver X-β receptor (LXRβ) agonists, and
may be useful for treating or preventing pathologies related thereto. Such pathologies include, but are not limited to, inflammatory diseases and diseases characterized by defects in cholesterol and
lipid metabolism, such as Alzheimer's disease.
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4-alkynyl imidazole derivative and medicine comprising same as active ingredient
(Fri, 12 May 2017)
<p id="p-0001" num="0000">There are provided 4-alkynylimidazole derivatives represented by the following general formula (I) or pharmaceutically acceptable salts thereof; the derivatives have a
superior EP4 receptor antagonistic action and are useful as pharmaceuticals for the treatment of diseases associated with the EP4 receptor, for example, as anti-inflammatory and/or analgesic drugs
for inflammatory diseases and diseases that involve various kinds of pains, and further as pharmaceuticals for the treatment of immune diseases that result from inflammations as evoked by tissue
destruction due to the activation of Th1 cells and/or Th17 cells:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="53.42mm"
wi="69.85mm" file="US09855257-20180102-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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4,5,6,7-TETRAHYDRO-1H-IMIDAZO[4,5-C]PYRIDINE AND 1,4,5,6,7,8-HEXAHYDROIMIDAZO[4,5-D]AZEPINE DERIVATIVES AS JANUS KINASE INHIBITORS
(Fri, 12 May 2017)
There are provided compounds of formula (I), wherein X, Ak, s, L, Q, R1 and R2 have meanings given in the description, which compounds have antiinflammatory activity (e.g. through inhibition of one
or more of members of the JAK family) and have use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the
lung, eye and intestines.
>> Read More

4,5,6,7-TETRAHYDRO-1H-IMIDAZO[4,5-C]PYRIDINE AND 1,4,5,6,7,8-HEXAHYDROIMIDAZO[4,5-D]AZEPINE DERIVATIVES AS JANUS KINASE INHIBITORS
(Fri, 12 May 2017)
There are provided compounds of formula I, wherein X, Ak, s, A, R1 and R2 have meanings given in the description, which compounds have antiinflammatory activity (e.g. through inhibition of one or
more of members of the JAK family) and have use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the
lung, eye and intestines.
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BIOLOGICALLY ACTIVE OLIGONUCLEOTIDES CAPABLE OF MODULATING THE IMMUNE SYSTEM
(Thu, 11 May 2017)
The present invention relates to methods of identifying oligonucleotides capable of modulating the immune system in a mammalian subject, comprising analysis of which tertiary structural type said
oligonucleotide adopts, in phosphate-buffered saline solution. Further, the invention provides oligonucleotides identifiable by the methods of the invention and to their use in methods of treating
diseases, such as inflammatory diseases, autoimmune diseases, infectious diseases, neurodegenerative diseases and cancer.
>> Read More

METHOD FOR PRODUCING INDOLE COMPOUND
(Thu, 11 May 2017)
The present invention aims to provide a new method for producing an indole compound or a salt thereof, which has an ITK inhibitory action, and is useful for the prophylaxis or treatment of
inflammatory disease. The present invention is a method for producing N-[2-(6,6-dimethyl-4,5,6,7-tetrahydro-1H-indazol-3-yl)-1H-indol-6-yl]-N-methyl-(2S)-2-(morpholin-4-yl)propanamide, which
comprises a step of reacting with
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DENDRIMER COMPOSITIONS AND USE IN TREATMENT OF NECROTIZING ENTEROCOLITIS AND OTHER GASTROINTESTINAL DISORDERS
(Fri, 05 May 2017)
<p id="p-0001" num="0000">A dendrimer formulation, such as a PAMAM dendrimer or a multiarm PEG polymeric formulation has been developed for oral administration to the gastrointestinal tract for
treatment of inflammatory diseases associated with infection or cancer. In the preferred embodiment, the dendrimers are in the form of dendrimer nanoparticles comprising poly(amidoamine) (PAMAM)
hydroxyl-terminated dendrimers covalently linked to at least one therapeutic, prophylactic or diagnostic agent for treatment of one or more symptoms of necrotizing enterocolitis.</p>
>> Read More

BET-PROTEIN INHIBITING 3,4-DIHYDROPYRIDO[2,3-B]PYRAZINONES WITH META-SUBSTITUTED AROMATIC AMINO- OR ETHER GROUPS
(Fri, 05 May 2017)
<p id="p-0001" num="0000">The present invention relates to BET protein-inhibitory, especially BRD4-inhibitory 3,4-dihydropyrido[2,3-b]pyrazinones with a meta-substituted aromatic amino or ether
group of the general formula (I)</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="39.03mm" wi="62.57mm"
file="US20170121322A1-20170504-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">in which A, X, Y,
R<sup>1</sup>, R<sup>2</sup>, R<sup>3</sup>, R<sup>4</sup>, R<sup>5</sup>, R<sup>6 </sup>and n are each as defined in the
description, to pharmaceutical compositions comprising the compounds according to the invention, and to the prophylactic and therapeutic use thereof in the case of hyperproliferative disorders,
especially in the case of tumour disorders.</p> <p id="p-0004" num="0000">Furthermore, this invention relates to the use of BET protein inhibitors in viral infections, in
neurodegenerative disorders, in inflammatory diseases, in atherosclerotic disorders and in male fertility control.</p>
>> Read More

Lanthionine synthetase C-like 2-based therapeutics
(Fri, 05 May 2017)
<p id="p-0001" num="0000">Provided are compounds that target the lanthionine synthetase C-like protein 2 pathway. The compounds can be used to treat a number of conditions, including infectious
disease, autoimmune disease, diabetes, and a chronic inflammatory disease.</p>
>> Read More

DENDERIMER COMPOSITIONS AND USE IN TREATMENT OF NECROTIZING ENTEROCOLITIS AND OTHER GASTROINTESTINAL DISORDERS
(Fri, 05 May 2017)
A dendrimer formulation, such as a PAMAM dendrimer or a multiarm PEG polymeric formulation has been developed for oral administration to the gastrointestinal tract for treatment of inflammatory
diseases associated with infection or cancer. In the preferred embodiment, the dendrimers are in the form of dendrimer nanoparticles comprising poly(amidoamine) (PAMAM) hydroxyl-terminated dendrimers
covalently linked to at least one therapeutic, prophylactic or diagnostic agent for treatment of one or more symptoms of necrotizing enterocolitis.
>> Read More

Diaryl urea derivatives as p38 kinase inhibitors
(Fri, 05 May 2017)
There are provided compounds of formula I, wherein R<sp>1A</sp> to R<sp>1E</sp>, R<sp>2</sp> to R<sp>4</sp>, R<sp>5a</sp>, L and X1 to X3
have meanings given in the description, which compounds have antiinflammatory activity (e.g. through inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase
enzymes; Syk kinase; and members of the Src family of tyrosine kinases) and have use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases,
including inflammatory diseases of the lung, eye and intestines.
>> Read More

4-(4-(4-phenylureido-naphthalen-1-yl)oxy-pyridin-2-yl)amino-benzoic acid derivative as p38 kinase inhibitor
(Fri, 05 May 2017)
There is provided a compound of formula I, which compound has antiinflammatory activity (e.g. through inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase
enzymes; Syk kinase; and members of the Src family of tyrosine kinases) and has use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases,
including inflammatory diseases of the lung, eye and intestines.
>> Read More

6-[5-AMINO-6-(2-ETHOXYETHOXY)-IMIDAZO[4,5-B]PYRIDIN-3-YL]-NICOTINONITRILE DERIVATIVES AND THEIR USE AS IRAK INHIBITORS
(Fri, 28 Apr 2017)
The present invention discloses compounds according to Formula (I): wherein R1, R2, and Cy are as defined herein. The present invention relates to compounds inhibiting IRAK family kinases, methods
for their production, pharmaceutical compositions comprising the same, and methods of treatment using the same, for the prophylaxis and/or treatment of inflammatory diseases, autoimmune diseases
and/or proliferative diseases by administering the compound of the invention.
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NEW DERIVATIVES OF LICOFELONE
(Fri, 28 Apr 2017)
The present invention relates to novel derivatives, preferably prodrugs, of licofelone suitable as a medicament, preferably in the treatment and/or prevention of systemic diseases, autoimmune
diseases or inflammatory diseases. Further, the invention relates to a pharmaceutical composition comprising the novel compounds. The compounds are of formula (I) where L is a linear organic residue
comprising 2 to 30 carbon atoms, and R is -OH or -OOCR', wherein -OOCR' is a carboxylate group which is hydrolyzable during small intestinal transit. Formula (I)
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Small Molecule Transcription Modulators of Bromodomains
(Fri, 21 Apr 2017)
<p id="p-0001" num="0000">This disclosure relates generally to compounds and compositions comprising one or more indole analogs. These compounds are useful for treating diseases associated with
NF-kB and p53 activity, such as cancer and inflammatory diseases.</p>
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CONFORMATIONALLY CONSTRAINED MACROCYCLIC COMPOUNDS AS PIN1 MODULATORS
(Fri, 21 Apr 2017)
Conformationally constrained macrocyclic compounds of formula (I), including substituents E, G, and Q, as defined in the description and the claims, and salts thereof, have the property to modulate
the activity of the peptidyl-prolyl cis/trans isomerases Pin1. Thus, these compounds and pharmaceutical compositions containing said compounds may be useful in the treatment and/or prevention of
diseases or conditions in the area of proliferative disorders and diseases, such as e.g. cancer, inflammatory diseases, transplant rejection, viral infections, osteolytic bone diseases, cardiac
diseases, cardiovascular diseases, respiratory diseases, acute neurological diseases, neurodegenerative diseases, immune disorders, and lymphoproliferative theileriosis.
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CONFORMATIONALLY CONSTRAINED MACROCYCLIC COMPOUNDS
(Fri, 21 Apr 2017)
Formula (I); Conformationally constrained macrocyclic compounds of formula (I), including substituents E with at least one ester moiety, G and Q, as defined in the description and the claims, and
salts thereof, can be metabolized to compounds that have the property to modulate the activity of the peptidyl-prolyl cis/trans isomerase Pin1. In addition, they show antiproliferative activity on
various cancer cell lines. Thus, these compounds and pharmaceutical compositions containing said compounds may be useful in the treatment and/or prevention of diseases or conditions in the area of
proliferative disorders and diseases, such as e.g. cancer, inflammatory diseases, transplant rejection, viral infections, osteolytic bone diseases, cardiac diseases, cardiovascular diseases,
respiratory diseases, acute neurological diseases, neurodegenerative diseases, immune disorders, and lymphoproliferative theileriosis.
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CONFORMATIONALLY CONSTRAINED MACROCYCLIC COMPOUNDS AS PIN1 MODULATORS
(Fri, 21 Apr 2017)
Conformationally constrained macrocyclic compounds of formula (I), including substituents E, G, and Q, as defined in the description and the claims, and salts thereof, have the property to modulate
the activity of the peptidyl-prolyl cis/trans isomerases Pin1. Thus, these compounds and pharmaceutical compositions containing said compounds may be useful in the treatment and/or prevention of
diseases or conditions in the area of proliferative disorders and diseases, such as e.g. cancer, inflammatory diseases, transplant rejection, viral infections, osteolytic bone diseases, cardiac
diseases, cardiovascular diseases, respiratory diseases, acute neurological diseases, neurodegenerative diseases, immune disorders, and lymphoproliferative theileriosis.
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CONFORMATIONALLY CONSTRAINED MACROCYCLIC COMPOUNDS
(Fri, 21 Apr 2017)
Conformationally constrained macrocyclic compounds of formula (I), including substituents E with at least one ester moiety, G and Q, as defined in the description and the claims, and salts thereof,
can be metabolized to compounds that have the property to modulate the activity of the peptidyl-prolyl cis/trans isomerase Pin1. In addition, they show antiproliferative activity on various cancer
cell lines. Thus, these compounds and pharmaceutical compositions containing said compounds may be useful in the treatment and/or prevention of diseases or conditions in the area of proliferative
disorders and diseases, such as e.g. cancer, inflammatory diseases, transplant rejection, viral infections, osteolytic bone diseases, cardiac diseases, cardiovascular diseases, respiratory diseases,
acute neurological diseases, neurodegenerative diseases, immune disorders, and lymphoproliferative theileriosis.
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Bet-protein inhibiting 3,4-dihydropyrido[2,3-b]pyrazinones with meta-substituted aromatic amino- or ether groups
(Thu, 20 Apr 2017)
The invention relates to BET-protein-inhibiting, in particular BRD4-inhibiting 3,4-dihydropyrido[2,3-b]pyrazinones with meta-substituted aromatic amino or ether groups of general formula (I), in
which A, X, Y, R1, R2, R3, R4, R5, R6, and n have the meanings indicated in the description, pharmaceutical agents containing the claimed compounds, and the prophylactic and therapeutic use of said
pharmaceutical agents in the case of hyperproliferative diseases, in particular in the case of tumor diseases. The invention further relates to the use of BET protein inhibitors in the case of viral
infections, neurodegenerative diseases, inflammatory diseases, and atherosclerotic diseases and in male fertility control.
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BINDING INHIBITOR BETWEEN TCTP DIMER TYPE IGE-DEPENDENT HISTAMINE RELEASING FACTOR AND RECEPTOR THEREOF, AND USE THEREOF
(Thu, 20 Apr 2017)
The present invention relates to a receptor-binding domain of an IgE-dependent histamine releasing factor (HRF), and a use thereof and, more specifically, ascertains, as an HRF framework region, an
FL domain and an H2 domain which bind to a receptor of an HRF existing in a cell membrane, ascertains the C-terminus of the HRF, and ascertains that a material binding thereto inhibits IL-8
secretion, thereby determining that the FL and H2 domains and the C-terminus can be utilized in: the development of a therapeutic agent for and prevention of HRF-related diseases including malaria
and inflammatory diseases such as asthma, bronchitis, chronic obstructive pulmonary disease, bronchiectasis, rhinitis, atopic dermatitis, hives, hay fever, conjunctivitis, anaphylactic allergic
diseases, pneumonia, arthritis, nephritis, psoriasis, dermatitis, Crohn's disease, enteritis, gingivitis, arteriosclerosis, coronary arteritis, hepatitis, Behcet's disease, bladder cancer,
prostatitis, pyelonephritis, glomerulonephritis, osteomyelitis, thyroiditis, uveitis, abdominal cavity inflammation, meningitis, pulmonary fibrosis and rheumatoid arthritis; and a method for
screening for the HRF-related diseases.
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COMPOSITION COMPRISING CYCLODEXTRIN AND BUDESONIDE DERIVATIVES FOR THE TREATMENT AND PROPHYLAXIS OF PULMONARY INFLAMMATIONS
(Thu, 13 Apr 2017)
The present invention relates to novel and useful pharmaceutical compositions formulated with a cyclodextrin compound and a budesonide derivative for the treatment and/or prevention of pulmonary
inflammatory disease. The present invention also relates to a novel and useful analytical technique for the detection and the quantification of ΗΡ-β-CD in solution. More specifically, the present
invention relates to the use of a validated 1H NMR analysis for the detection and quantification of cyclodextrins directly in pharmaceutical formulations without any extraction or separation steps
for liquid formulations.
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BIOMARKERS AND METHODS FOR MEASURING AND MONITORING AXIAL SPONDYLOARTHRITIS ACTIVITY
(Fri, 07 Apr 2017)
<p id="p-0001" num="0000">Biomarkers useful for diagnosing and assessing inflammatory disease activity, for prediction of risk for progressive spinal and joint damage, in particular for axial
spondyloarthritis (axSpA) and ankylosing spondylitis (AS), and for generating a dataset are provided, along with kits for measuring expression of the biomarkers. The invention also provides
predictive models, based on the biomarkers, as well as computer systems, and software embodiments of the models for scoring and optionally classifying samples.</p>
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BIOMARKERS AND METHODS FOR ASSESSING RESPONSE TO INFLAMMATORY DISEASE THERAPY WITHDRAWAL
(Fri, 07 Apr 2017)
Provided herein are methods for assessing response to inflammatory disease therapy. The methods include placing a subject on a therapeutic regimen and subsequently performing an immunoassay to
generate a score based on quantitative data for expression of biomarkers relating to inflammatory biomarkers. The methods further include recommending that the subject either remains on the
therapeutic regimen, or is removed from the therapeutic regimen, based on the score.
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Combinations of the BTK inhibitor GS-4059 with inhibitors selected from a JAK, ASK1, BRD and/or MMP9 inhibitor to treat cancer, allergic disorders, autoimmune diseases or inflammatory diseases
(Fri, 07 Apr 2017)
Provided herein are methods that relate to a therapeutic strategy for treatment of cancer, and allergic, autoimmune, and inflammatory disorders including hematological malignancies. In particular,
the methods include administration of a BTK inhibitor and with one or more inhibitor. For example, the one or more inhibitor may be a JAK inhibitor, a ASK1 inhibitor, a BRD4 inhitibor or an MMP9
inhibitor.
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Amyloid beta peptides as therapy for multiple sclerosis
(Wed, 05 Apr 2017)
<p id="p-0001" num="0000">The invention provides methods for treating inflammatory diseases by administering to the subject an effective amount of an amyloid beta peptide, where the dose is
effective to suppress or prevent initiation, progression, or relapses of disease, including the progression of established disease.</p>
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Amine derivatives as potassium channel blockers
(Fri, 31 Mar 2017)
<p id="p-0001" num="0000">The present invention relates to compounds useful in the modulation of potassium channel activity in cells, in particular the activity of Kv1.3 channels found in T
cells. The invention also relates to the use of these compounds in the treatment or prevention of autoimmune and inflammatory diseases, including multiple sclerosis, pharmaceutical compositions
containing these compounds and methods for their preparation.</p>
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BENZIMIDAZOLES FOR USE IN THE TREATMENT OF CANCER AND INFLAMMATORY DISEASES
(Fri, 31 Mar 2017)
Provided herein are methods for treating, preventing, or ameliorating one or more symptoms of a condition, disorder, or disease mediated by a lipid kinase or a protein kinase with benzimidazoles, for
example, of Formula I or II, and pharmaceutical compositions thereof. Also provided herein are benzimidazoles, and pharmaceutical compositions thereof; and methods of their use for treating,
preventing, or ameliorating one or more symptoms of a proliferative disease.
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METHODS FOR THE TREATMENT OF CANCER AND INFLAMMATORY DISEASES USING CEREBLON AS A PREDICTOR
(Fri, 31 Mar 2017)
Uses of the protein cereblon as a predictor of clinical sensitivity to cancer, inflammatory diseases, and patient response to drug treatment.
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PURINONE COMPOUNDS AS KINASE INHIBITORS
(Thu, 30 Mar 2017)
Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. In addition, reversible inhibitors of Btk are also
described. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the
treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.
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CARBORANE COMPOUNDS AND METHODS OF USE THEREOF
(Fri, 24 Mar 2017)
Disclosed herein are compounds comprising dicarba-closo-dodecaborane. The compounds can be, for example, estrogen receptor beta (ERβ) agonists. In some examples, the compounds can be selective ERβ
agonists. Also provided herein are methods of treating, preventing, or ameliorating cancer in a subject, suppressing tumor growth in a subject, treating an inflammatory disease in a subject, treating
a neurodegenerative disease in a subject, treating a psychotropic disorder in a subject, or a combination thereof, by administering to a subject a therapeutically effective amount of one or more of
the compounds or compositions described herein, or a pharmaceutically acceptable salt thereof.
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COMPOUNDS FOR THE MODULATION OF RIP2 KINASE ACTIVITY
(Fri, 24 Mar 2017)
The present invention relates to compounds, compositions, combinations and medicaments containing said compounds and processes for their preparation. The invention also relates to the use of said
compounds, combinations, compositions and medicaments, for example as inhibitors of the activity of RIP2 kinase, including degrading RIP2 kinase, the treatment of diseases and conditions mediated by
the RIP2 kinase, in particular for the treatment of inflammatory diseases or conditions.
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Carborane compounds and methods of use thereof
(Fri, 24 Mar 2017)
Disclosed herein are compounds comprising dicarba-closo-dodecaborane. The compounds can be, for example, estrogen receptor beta (ERβ) agonists. In some examples, the compounds can be selective ERβ
agonists. Also provided herein are methods of treating, preventing, or ameliorating cancer in a subject, suppressing tumor growth in a subject, treating an inflammatory disease in a subject, treating
a neurodegenerative disease in a subject, treating a psychotropic disorder in a subject, or a combination thereof, by administering to a subject a therapeutically effective amount of one or more of
the compounds or compositions described herein, or a pharmaceutically acceptable salt thereof.
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Novel 2-phenylbenzofuran derivative or pharmaceutically acceptable salt thereof, production method for same and pharmaceutical composition for preventing or treating inflammatory disease comprising same as active ingredient
(Thu, 23 Mar 2017)
The present invention relates to a novel 2-phenylbenzofuran derivative or a pharmaceutically acceptable salt thereof, to a production method for same and to a pharmaceutical composition for
preventing or treating an inflammatory disease comprising same as an active ingredient, and the novel 2-phenylbenzofuran derivative or the pharmaceutically acceptable salt thereof according to the
present invention is outstandingly effective in suppressing NO, IL-6 and TNF-alpha due to macrophages, and therefore can advantageously be used in a pharmaceutical composition for preventing or
treating an inflammatory disease.
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TRICYCLIC COMPOUND AND JAK INHIBITOR
(Thu, 23 Mar 2017)
Novel tricyclic compounds which have JAK inhibitory activities are useful for prevention, treatment or improvement of autoimmune diseases, inflammatory diseases and allergic diseases are provided.
Novel tricyclic compound represented by the formula (I), the formula (II) or the formula (III) (wherein : each of A 1 , A 2 and A 3 is a cyclohexane-1,4-diyl group or the like; each of L 1 , L 2 and
L 3 is a methylene group or the like; each of X 1 and X 3 is O or NH; each of R 1 and R 3 is a cyano C 1-6 haloalkyl group or the like; and R 2 is an aromatic heterocyclic group), a tautomer or
pharmaceutically acceptable salt of the compound or a solvate thereof.
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Biomarkers and Methods for Measuring and Monitoring Inflammatory Disease Activity
(Fri, 17 Mar 2017)
<p id="p-0001" num="0000">Biomarkers useful for diagnosing and assessing inflammatory disease are provided, along with kits for measuring their expression. The invention also provides
predictive models, based on the biomarkers, as well as computer systems, and software embodiments of the models for scoring and optionally classifying samples. The biomarkers include at least two
biomarkers selected from the DAIMRK group and the score is a disease activity index (DAI).</p>
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IL-17A/F HETEROLOGOUS POLYPEPTIDES AND THERAPEUTIC USES THEREOF
(Fri, 17 Mar 2017)
<p id="p-0001" num="0000">The present invention is directed to a novel naturally occurring human cytokine that is comprised of a heterodimer of interleukin-17 and interleukin-17F designated
herein as interleukin 17A/F (IL-17A/F). Also provided herein are vectors and host cells comprising those nucleic acid sequences, chimeric polypeptide molecules comprising the polypeptides of the
present invention fused to heterologous polypeptide sequences, specific antibodies which bind to the polypeptides of the present invention and to methods for producing the polypeptides of the present
invention. Further provided herein are methods for treating degenerative cartilaginous disorders and other inflammatory diseases.</p>
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Alanine derivative
(Thu, 16 Mar 2017)
The present invention provides a compound which is: tert-butyl N-[2-{4-[6-amino-5- (2,4-difluorobenzoyl)-2-oxopyridin-1(2H)-yl]-3,5-difluorophenyl}ethyl)-L-alaninate or a salt, hydrate or solvate
thereof. The present invention also provides a pharmaceutical composition comprising the compound together with one or more pharmaceutically acceptable carriers and/or excipients. The compound and
composition are useful for inhibiting the activity of a p38 MAP kinase enzyme. As such they may be used in the treatment of a autoimmune or inflammatory disease, or a cell proliferative disease. In
addition, the invention provides an acid produced by hydrolysis of the ester group of the compound of the invention. The acid is N-[2-{4-[6-amino-5-(2,4-difluorobenzoyl)-2-
oxopyridin-1(2H)-yl]-3,5-difluorophenyl}ethyl)-L-alanine.
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SALTS AND SOLID FORM OF A BTK INHIBITOR
(Fri, 10 Mar 2017)
<p id="p-0001" num="0000">Disclosed herein are processes for preparing
2-[(3R)-3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4-[4-(oxetan-3-yl)piperazin-1-yl]pent-2-enenitrile free base (compound (I)), salts of
compound (I) and solid state form of said salts. Also disclosed herein are pharmaceutical compositions comprising such salts and solid state form thereof and methods of treating cancer, autoimmune,
and inflammatory diseases using compound (I) or a pharmaceutically acceptable salt thereof.</p>
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Fumarate analogs and uses thereof
(Fri, 10 Mar 2017)
<p id="p-0001" num="0000">Aspects of the present disclosure include compounds that find use for the treatment of a variety of autoimmune and inflammatory diseases and disorders. Embodiments of
the present disclosure also relate to pharmaceutical compositions that include these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for
preparing these compounds and intermediates useful in these processes.</p>
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WITHAFERIN A ANALOGS AND USES THEREOF
(Fri, 10 Mar 2017)
<p id="p-0001" num="0000">The present invention provides a novel class of withanolides that have been isolated from <i>W. somnifera </i>under aeroponic conditions or produced
semi-synthetically from withanolide natural products. The invention also provides pharmaceutical compositions thereof and methods for using the same in proliferative diseases, neurodegenerative
diseases, autoimmune, and inflammatory diseases.</p>
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AGENTS FOR USE IN THE TREATMENT OF CARDIOVASCULAR AND INFLAMMATORY DISEASES STRUCTURALLY BASED ON 4(1 H)-QUINOLONE
(Fri, 10 Mar 2017)
<p id="p-0001" num="0000">The present invention provides a compound of formula I, a tautomer thereof, or a pharmaceutically acceptable salt or N-oxide thereof for use in the treatment or
prevention of cardiovascular disease or of an inflammatory disease or condition:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001"
he="27.86mm" wi="53.17mm" file="US20170066722A1-20170309-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <ul id="ul0001" list-style="none"> <li
id="ul0001-0001" num="0000"> <ul id="ul0002" list-style="none"> <li id="ul0002-0001" num="0000">wherein:</li> <li id="ul0002-0002" num="0000">V is N or
CR<sub>3</sub>;</li> <li id="ul0002-0003" num="0000">X is N or CR<sub>4</sub>;</li> <li id="ul0002-0004" num="0000">Y is N or
CR<sub>5</sub>;</li> <li id="ul0002-0005" num="0000">Z is N or CR<sub>6</sub>;</li> <li id="ul0002-0006" num="0000">B is
—(C═O)R<sub>1</sub>, a 5- to 10-membered heteroaryl group, or a group</li> <li id="ul0002-0007" num="0000">-L′″-NRR′, wherein R and R′ are the same or different and each
represents a hydrogen atom, a C<sub>1</sub>-C<sub>6 </sub>alkyl group or a C<sub>1</sub>-C<sub>6 </sub>haloalkyl group;</li> <li
id="ul0002-0008" num="0000">R<sub>1 </sub>is a 5- to 10-membered heterocyclyl group, or —OR′, wherein R′ is a hydrogen atom, a C<sub>1</sub>-C<sub>6 </sub>alkyl
group or a C<sub>1</sub>-C<sub>6 </sub>haloalkyl group, or R<sub>1 </sub>is a proteinogenic α amino acid, which is linked to the carbonyl moiety in the compound of
formula (I) via the α amino group, which amino acid is optionally esterified at the α carboxylic acid group with a C<sub>1</sub>-C<sub>6 </sub>alkyl group or a
C<sub>6</sub>-C<sub>10 </sub>aryl group, or R<sub>1 </sub>is —NR″R′″, —NR<sup>IV</sup>-L′″-CONR″R′″, or —NR<sup>IV</sup>-L′″-COOR, wherein
R, R″, R′″ and R<sup>IV </sup>are the same or different and each represents a hydrogen atom, a C<sub>1</sub>-C<sub>6 </sub>alkyl group or a
C<sub>1</sub>-C<sub>6 </sub>haloalkyl group;</li> <li id="ul0002-0009" num="0000">either (a) W is N and R<sub>9 </sub>and R<sub>2
</sub>together form a bond, or (b) W is CR<sub>8</sub>, R<sub>8 </sub>and R<sub>9 </sub>together form a bond and R<sub>2 </sub>is a hydrogen
atom, or a C<sub>1</sub>-C<sub>6 </sub>alkyl, C<sub>1</sub>-C<sub>6 </sub>haloalkyl, C<sub>6</sub>-C<sub>10 </sub>aryl, 5- to
10-membered heteroaryl, 5- to 10-membered heterocyclyl, -L′-A<sub>2</sub>, C<sub>3</sub>-C<sub>10 </sub>cycloalkyl, or —COOR′ group, wherein R′ is a hydrogen atom
or C<sub>1</sub>-C<sub>6 </sub>alkyl group, or, when Z is a moiety CR<sub>6</sub>, R<sub>2 </sub>may form, together with R<sub>6 </sub>and
the carbon and nitrogen atoms which connect R<sub>2 </sub>and R<sub>6 </sub>in the formula (I), a 5- to 6-membered heterocyclic ring;</li> <li id="ul0002-0010"
num="0000">R<sub>3 </sub>is a hydrogen atom, a halogen atom, or a hydroxy, C<sub>1</sub>-C<sub>6 </sub>alkyl, C<sub>1</sub>-C<sub>6
</sub>alkoxy, C<sub>1</sub>-C<sub>6 </sub>haloalkyl, C<sub>1</sub>-C<sub>6 </sub>haloalkoxy, nitro, or —NR′R″ group, wherein R′ and R″ are the
same or different and each represent a hydrogen atom or C<sub>1</sub>-C<sub>6 </sub>alkyl group;</li> <li id="ul0002-0011" num="0000">R<sub>4 </sub>and
R<sub>5 </sub>are the same or different and each represent a hydrogen atom, a halogen atom, or a hydroxyl, C<sub>1</sub>-C<sub>8 </sub>alkyl,
C<sub>1</sub>-C<sub>8 </sub>haloalkyl, C<sub>1</sub>-C<sub>6 </sub>alkoxy, C<sub>1</sub>-C<sub>6 </sub>haloalkoxy, nitro,
—NR′R″, —CO<sub>2</sub>R′″, C<sub>6</sub>-C<sub>10 </sub>aryl, 5- to 10-membered heteroaryl, 5 to 10-membered heterocyclyl, or
—CO—(C<sub>1</sub>-C<sub>6 </sub>alkyl) group, wherein R′, R″ and R′″ are the same or different and each represent a hydrogen atom or C<sub>1</sub>-C<sub>6
</sub>alkyl group, or R<sub>4 </sub>and R<sub>5 </sub>and the carbon atoms bonded to R<sub>4 </sub>and R<sub>5 </sub>together form a 5- to
6-membered heterocyclic ring;</li> <li id="ul0002-0012" num="0000">R<sub>6 </sub>is a hydrogen atom, a halogen atom, or a C<sub>1</sub>-C<sub>6
</sub>alkyl, C<sub>1</sub>-C<sub>6 </sub>haloalkyl, C<sub>1</sub>-C<sub>6 </sub>alkoxy, C<sub>1</sub>-C<sub>6
</sub>haloalkoxy or —CO<sub>2</sub>R′ group, wherein R′ is hydrogen or C<sub>1</sub>-C<sub>6 </sub>alkyl, or, when W is a moiety CR<sub>8</sub>,
R<sub>6 </sub>may form, together with R<sub>2 </sub>and the carbon and nitrogen atoms which connect R<sub>6 </sub>and R<sub>2 </sub>in the formula (I),
a 5- to 6-membered heterocyclic ring;</li> <li id="ul0002-0013" num="0000">R<sub>7 </sub>is a hydrogen atom, a halogen atom, or a C<sub>1</sub>-C<sub>6
</sub>alkyl, or C<sub>1</sub>-C<sub>6 </sub>haloalkyl group,</li> <li id="ul0002-0014" num="0000">A<sub>2 </sub>represents a
C<sub>6</sub>-C<sub>10 </sub>aryl or 5- to 10-membered heteroaryl group;</li> <li id="ul0002-0015" num="0000">L′, and L′″ are the same or different and each
represent a C<sub>1</sub>-C<sub>6 </sub>alkylene, C<sub>2</sub>-C<sub>6 </sub>alkenylene, or C<sub>2</sub>-C<sub>6
</sub>alkynylene group;</li> <li id="ul0002-0016" num="0000">said aryl, heteroaryl, cycloalkyl and heterocyclyl groups being unsubstituted or substituted with one or more
substituents selected from halogen, hydroxy, C<sub>1</sub>-C<sub>4 </sub>alkyl, C<sub>1</sub>-C<sub>4 </sub>hydroxyalkyl,
C<sub>1</sub>-C<sub>4 </sub>alkoxy, C<sub>1</sub>-C<sub>4 </sub>haloalkyl, C<sub>1</sub>-C<sub>4 </sub>haloalkoxy, —SOR,
—SO<sub>2</sub>R, —NR′R″, —NR′(C═O)R″, —COOR, nitro and cyano substituents, wherein R, R′ and R″ are the same or different and each represents a hydrogen atom or
C<sub>1</sub>-C<sub>4 </sub>alkyl group.</li> </ul> </li> </ul> </p>
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